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Chemical Structure| 842133-18-0 Chemical Structure| 842133-18-0
Chemical Structure| 842133-18-0

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CAS No.: 842133-18-0

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Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50 values of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.

Synonyms: JNJ 28431754; TA-7284; JNJ-24831754

4.5 *For Research Use Only !

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Product Citations

Product Citations

Hasan, Ahasanul ; Zerin, Farzana ; Menon, Sreelakshmi N ; Alam, Md Ashraful ; Hasan, Raquibul ;

Abstract: Canagliflozin, a sodium glucose co-transporter 2 (SGLT2) inhibitor, is reported to produce beneficial cardiovascular effects including a reduction in arterial contractility, and blood pressure. However, whether canagliflozin could directly relax resistance mesenteric arteries, underlying molecular mechanism and its role in regulating systemic blood pressure remain unclear. Here, we investigated the mechanism of regulation of small mesenteric artery contractility and its relevance for blood pressure regulation. Our pressure myography data showed that canagliflozin application rapidly produces a concentration-dependent vasodilation in mesenteric arteries. Such vasodilation was inhibited by concurrent inhibition of smooth muscle cell voltage-gated Kt channels KV1.5 (by 1 mM DPO-1), KV2.1 (by 100 nM guangxitoxin), and KV7 (by 10 mM linopirdine) but not by the inhibition of small-, intermediate-, and large-conductance Ca2t-activated Kt channels (SKCa by 1 mM apamin, IKCa 10 mM TRAM-34, and BKCa by 10 mM paxilline, respectively), ATP-sensitive (KATP) channels (by 10 mM glibenclamide), or SERCA pump (by 0.1 mM thapsigargin). Inhibition of SGLTs (by 1 mM phlorizin or the inhibition of endothelial signaling did not alter canagliflozin-evoked vasodilation. Consistently, acute canagliflozin treatment (4 mg/kg body weight) lowered systemic blood pressure in vivo. Overall, our data suggests that canagliflozin stimulates KV1.5, KV2.1, and KV7 channels, leading to vasodilation and a reduction of systemic blood pressure.

Keywords: Canagliflozin ; Mesenteric arteries ; Voltage-gated Kt channels ; Vasorelaxation ; Blood pressure

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Product Details of Canagliflozin

CAS No. :842133-18-0
Formula : C24H25FO5S
M.W : 444.52
SMILES Code : FC1=CC=C(C2=CC=C(CC3=C(C=CC([C@@H]4O[C@@H]([C@H]([C@@H]([C@H]4O)O)O)CO)=C3)C)S2)C=C1
Synonyms :
JNJ 28431754; TA-7284; JNJ-24831754
MDL No. :MFCD18251436
InChI Key :XTNGUQKDFGDXSJ-ZXGKGEBGSA-N
Pubchem ID :24812758

Safety of Canagliflozin

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H318-H361
Precautionary Statements:P201-P202-P280-P281-P305+P351+P338-P308+P313-P310-P405-P501

Isoform Comparison

Biological Activity

Target
  • SGLT2

    mSGLT2, IC50:2 nM

    hSGLT2, IC50:3.7 nM

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02053116 Type 2 Diabetes Mellitus Phase 2 Terminated(On 25April2014, stu... More >>dy was terminated before any dosing due to an AE of safety concern that occurred in protocol B1731003 with the same drug.) Less << - United States, Florida ... More >> Pfizer Investigational Site DeLand, Florida, United States, 32720 Less <<
NCT00650806 - Completed - -
NCT01273558 Diabetes Mellitus, Type 2 PHASE1 COMPLETED 2025-07-11 Neuss, Germany
NCT01756404 Healthy Phase 1 Completed - United States, Florida ... More >> Miramar, Florida, United States Less <<
NCT00650806 Obesity Phase 2 Completed - -
NCT02920918 Heart Failure, Systolic ... More >> Diabetes Mellitus, Type 2 Less << Phase 4 Active, not recruiting March 2019 United States, Virginia ... More >> Virginia Commonwealth University Richmond, Virginia, United States, 23298 Less <<
NCT02681497 - Completed - Canada, Ontario ... More >> Western University London, Ontario, Canada, N6A 3K7 Less <<
NCT01714206 Healthy Phase 1 Completed - -
NCT01032629 Diabetes Mellitus, Type 2 ... More >> Cardiovascular Diseases Risk Factors Less << Phase 3 Completed - -
NCT01459094 Healthy Phase 1 Completed - -
NCT02737657 - Completed - Kuwait ... More >> Kuwait City, Kuwait Lebanon Amioun, Lebanon Beirut, Lebanon Nabatieh, Lebanon Saida, Lebanon Taalabya, Lebanon Tripoli, Lebanon United Arab Emirates Al Ain, United Arab Emirates Dubai, United Arab Emirates Less <<
NCT02220907 - Completed - -
NCT02220907 Type 2 Diabetes Mellitus Phase 3 Completed - Japan ... More >> Research site Chubu, Japan Research site Chugoku, Japan Research site Hokkaido, Japan Research site Kanto, Japan Research site Kyushu, Japan Research site Tohoku, Japan Less <<
NCT01032629 - Completed - -
NCT01463774 Healthy Phase 1 Completed - United States, Nebraska ... More >> Lincoln, Nebraska, United States Less <<
NCT02354222 Type 2 Diabetes Mellitus Phase 3 Completed - Japan ... More >> Reserch site Kanto, Japan Reserch site Kinki, Japan Reserch site Tohoku, Japan Less <<
NCT02354222 - Completed - -
NCT01665638 Healthy Phase 1 Completed - Germany ... More >> Neuss, Germany Less <<
NCT02846506 Healthy Phase 1 Completed - United States, Arizona ... More >> Tempe, Arizona, United States Less <<
NCT02851212 Healthy Phase 1 Completed - United States, Arizona ... More >> Tempe, Arizona, United States Less <<
NCT02694263 Diabetes Mellitus, Type 2 Phase 4 Recruiting September 2018 United Kingdom ... More >> University Hospitals of Leicester NHS Trust Recruiting Leicester, Leicestershire, United Kingdom, LE5 4PW Contact: Emer Brady, PhD ?? 0116248 ext 8959 ?? emer.brady@uhl-tr.nhs.uk ?? Contact: Natasha Wileman, MSc ?? 0116258 ext 8929 ?? natasha.wileman@uhl-tr.nhs.uk ?? University Hospitals Birmingham NHS Foundation Trust Recruiting Birmingham, West Midlands, United Kingdom, B15 2TH Contact: Wasim Hanif ?? 0121371 ext 4404 ?? wasim.hanif@uhb.nhs.uk ?? Contact: Deborah Smith ?? 0121371 ext 4707 ?? deborah.smith@uhb.nhs.uk Less <<
NCT00968812 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT00968812 - Completed - -
NCT03267576 Diabetes Mellitus, Type 2 Phase 4 Completed - Mexico ... More >> Consultorio Privado Guadalajara, Mexico, 44150 Investigación Clínica Especializada Guadalajara, Mexico, 44600 Consultorio Privado en Unidad de Patología Clínica Guadalajara, Mexico, 44650 Instituto Nacional de Ciencias Medicas y Nutrición Salvador Zubirán Mexico City, Mexico, 14080 Hospital Universitario 'Dr. Jose Eleuterio Gonzalez' Monterrey, Mexico, 64460 Less <<
NCT01787357 Healthy Phase 1 Completed - United States, Arizona ... More >> Tempe, Arizona, United States Less <<
NCT01916863 Healthy Subjects Phase 1 Completed - United States, California ... More >> Lexicon Investigational Site Chula Vista, California, United States, 91911 Less <<
NCT01106677 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01748526 Healthy Phase 1 Completed - India ... More >> Ahmedabad, India Less <<
NCT01759576 Renal Insufficiency ... More >> Healthy Less << Phase 1 Completed - United States, Florida ... More >> Orlando, Florida, United States United States, Minnesota Minneapolis, Minnesota, United States United States, Tennessee Knoxville, Tennessee, United States Less <<
NCT01381887 Diabetes Mellitus, Type 2 Phase 1 Completed - United States, California ... More >> Chula Vista, California, United States United States, Florida Miramar, Florida, United States United States, Ohio Cincinnati, Ohio, United States United States, Texas Dallas, Texas, United States San Antonio, Texas, United States Less <<
NCT02851095 Healthy Phase 1 Completed - United States, Nebraska ... More >> Lincoln, Nebraska, United States Less <<
NCT02865668 Healthy Phase 1 Completed - United States, Arizona ... More >> Tempe, Arizona, United States Less <<
NCT01106690 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT02220920 Type 2 Diabetes Mellitus Phase 4 Completed - Japan ... More >> Reserch site Chubu, Japan Reserch site Chugoku, Japan Reserch site Hokkaido, Japan Reserch site Kanto, Japan Reserch site Kinki, Japan Reserch site Kyushu, Japan Reserch site Tohoku, Japan Less <<
NCT02220920 - Completed - -
NCT02360774 - Completed - -
NCT01821027 Healthy Phase 1 Completed - -
NCT01483781 Diabetes Mellitus, Type 2 ... More >> Plasma Volume Less << Phase 1 Completed - Germany ... More >> Neuss, Germany Less <<
NCT01106677 - Completed - -
NCT01137812 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01137812 - Completed - -
NCT03136484 Diabetes Diab... More >>etes Mellitus, Type 2 Less << Phase 3 Completed - -
NCT02025907 - Completed - -
NCT01106690 - Completed - -
NCT02025907 Diabetes Mellitus, Type 2 Phase 4 Completed - -
NCT01106625 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT02360774 Type 2 Diabetes ... More >> Overweight Obesity Less << Phase 4 Completed - United States, Massachusetts ... More >> Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 Less <<
NCT01173549 Healthy Phase 1 Completed - United States, California ... More >> La Jolla, California, United States Less <<
NCT01106625 - Completed - -
NCT02462421 Diabetes Mellitus|Gout|Hyperur... More >>icemia Less << PHASE4 TERMINATED 2021-12-31 -
NCT01508182 Healthy Phase 1 Completed - United States, Arizona ... More >> Tempe, Arizona, United States Less <<
NCT01508195 Healthy Phase 1 Completed - United States, Nebraska ... More >> Lincoln, Nebraska, United States Less <<
NCT01756417 Healthy Phase 1 Completed - United States, New Jersey ... More >> Neptune, New Jersey, United States Less <<
NCT02009488 Diabetes Mellitus, Type 2 Phase 1 Completed - United States, California ... More >> San Diego, La Jolla, California, United States United States, Florida Gainesville, Florida, United States Less <<
NCT02039258 Healthy Volunteers Phase 1 Completed - United States, Nebraska ... More >> Lincoln, Nebraska, United States Less <<
NCT01106651 - Completed - -
NCT01106651 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01081834 - Completed - -
NCT01939496 - Completed - -
NCT01989754 Diabetes Mellitus, Type 2 ... More >> Albuminuria Less << Phase 4 Completed - -
NCT01939496 Diabetes Mellitus, Type 2 ... More >> Hypertension Less << Phase 4 Completed - -
NCT01733108 Healthy Phase 1 Completed - -
NCT01081834 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01809327 Diabetes Mellitus, Type 2 Phase 3 Completed - -
NCT01989754 - Completed - -
NCT02077803 Healthy Phase 1 Completed - United States, Arizona ... More >> Tempe, Arizona, United States Less <<
NCT02354235 - Completed - -
NCT02354235 Type 2 Diabetes Mellitus Phase 3 Completed - Japan ... More >> Reserch site Kanto, Japan Reserch site Kinki, Japan Reserch site Tohoku, Japan Less <<
NCT02071368 Healthy Phase 1 Completed - United States, Arizona ... More >> Tempe, Arizona, United States Less <<
NCT01281579 Healthy Phase 1 Completed - -
NCT01381900 Diabetes Mellitus, Type 2 Phase 3 Completed - China ... More >> Baotou, China Beijing, China Changchun, China Changsha, China Chengdu, China Chongqing, China Guangzhou, China Hangzhou, China Harbin, China Nanchang, China Nanjing, China Nanning, China Shanghai, China Shenyang, China Shiyan, China Siping, China Su Zhou, China Tianjin, China Wuxi, China Xi'An, China Malaysia Kota Bharu, Malaysia Pulau Pinang, Malaysia Selangor, Malaysia Vietnam Hanoi, Vietnam Ho Chi Minh, Vietnam Less <<
NCT01809327 - Completed - -
NCT02065791 Diabetes Mellitus, Type 2 ... More >> Diabetic Nephropathy Less << Phase 3 Active, not recruiting June 28, 2019 -
NCT01381900 - Completed - -
NCT01463228 Healthy Phase 1 Completed - United States, Nebraska ... More >> Lincoln, Nebraska, United States Less <<
NCT01454622 Healthy Phase 1 Completed - United States, Arizona ... More >> Tempe, Arizona, United States Less <<
NCT02404870 Diabetes PTH ... More >> Vitamin D Fibroblast Growth Factor (FGF23) Phosphate Less << Phase 1 Recruiting May 1, 2019 United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Recruiting Bethesda, Maryland, United States, 20892 Contact: For more information at the NIH Clinical Center contact Office of Patient Recruitment (OPR) ?? 800-411-1222 ext TTY8664111010 ?? prpl@cc.nih.gov Less <<
NCT01195324 Healthy Phase 1 Completed - Belgium ... More >> Merksem, Belgium Less <<
NCT01791231 Healthy Phase 1 Completed - Belgium ... More >> Merksem, Belgium Less <<
NCT01286103 Healthy Phase 1 Completed - -
NCT01128985 Diabetes Mellitus, Type 2 Phase 1 Completed - United States, Florida ... More >> Fort Myers, Florida, United States Miramar, Florida, United States Less <<
NCT02065752 Healthy Volunteers Phase 1 Completed - United States, Arizona ... More >> Tempe, Arizona, United States Less <<
NCT02227849 Type 2 Diabetes Mellitus Phase 4 Completed - Japan ... More >> Reserch site Chubu, Japan Reserch site Hokkaido, Japan Reserch site Kanto, Japan Reserch site Kinki, Japan Less <<
NCT01340664 Diabetes Mellitus, Type 2 Phase 2 Completed - -
NCT01518712 Healthy Phase 1 Completed - United States, Arizona ... More >> Tempe, Arizona, United States Less <<
NCT01340664 - Completed - -
NCT02622113 Type 2 Diabetes Mellitus Phase 4 Completed - Japan ... More >> Reserch site Chubu, Japan Reserch site Chugoku, Japan Reserch site Hokkaido, Japan Reserch site Kanto, Japan Reserch site Kinki, Japan Reserch site Kyushu, Japan Reserch site Tohoku, Japan Less <<
NCT02688075 - Completed - Canada, Alberta ... More >> Calgary, Alberta, Canada Edmonton, Alberta, Canada Canada, British Columbia Coquitlam, British Columbia, Canada Surrey, British Columbia, Canada Canada, Manitoba Winnipeg, Manitoba, Canada Canada, Ontario Brampton, Ontario, Canada Downsview, Ontario, Canada Guelph, Ontario, Canada London, Ontario, Canada Mississauga, Ontario, Canada Ohsweken, Ontario, Canada Ottawa, Ontario, Canada Smiths Falls, Ontario, Canada Toronto, Ontario, Canada Canada, Quebec Laval, Quebec, Canada Longueuil, Quebec, Canada Montreal, Quebec, Canada Saint-Jean-Sur-Richelieu, Quebec, Canada Sherbrooke, Quebec, Canada St Marc Des Carrieres, Quebec, Canada Toronto, Quebec, Canada Westmont, Quebec, Canada Canada, Saskatchewan Saskatoon, Saskatchewan, Canada Less <<
NCT02039245 Healthy Volunteers Phase 1 Completed - United States, New Jersey ... More >> Neptune, New Jersey, United States Less <<
NCT01064414 Diabetes Mellitus, Type 2 ... More >> Renal Insufficiency Less << Phase 3 Completed - -
NCT01294631 Healthy Phase 1 Completed - -
NCT01395927 Healthy Phase 1 Completed - United States, Kansas ... More >> Overland Park, Kansas, United States Less <<
NCT01340677 Healthy Phase 1 Completed - Belgium ... More >> Merksem, Belgium Less <<
NCT01064414 - Completed - -
NCT01714193 Healthy Phase 1 Completed - -
NCT03170518 Diabetes Mellitus, Type 2 Phase 3 Recruiting June 30, 2021 -
NCT01273571 Healthy Phase 1 Completed - -
NCT01343290 Healthy PHASE1 COMPLETED 2025-06-11 -
NCT02243202 Obesity Phase 2 Completed - United States, Arizona ... More >> Phoenix, Arizona, United States United States, California Walnut Creek, California, United States United States, Florida Jacksonville, Florida, United States United States, Idaho Meridian, Idaho, United States United States, Indiana Evansville, Indiana, United States United States, Kentucky Lexington, Kentucky, United States Louisville, Kentucky, United States United States, Louisiana New Orleans, Louisiana, United States United States, Massachusetts Milford, Massachusetts, United States United States, New York Manlius, New York, United States United States, Rhode Island Warwick, Rhode Island, United States United States, South Carolina Mt Pleasant, South Carolina, United States United States, Tennessee Nashville, Tennessee, United States United States, Texas Dallas, Texas, United States Odessa, Texas, United States United States, Virginia Norfolk, Virginia, United States United States, Wisconsin Wauwatosa, Wisconsin, United States Less <<
NCT02139943 - Completed - -
NCT02964585 Type 2 Diabetes Mellitus Phase 4 Recruiting May 2019 United States, District of Col... More >>umbia The George Washington University Medical Faculty Associates Recruiting Washington, District of Columbia, United States, 20037 Contact: Fiona Dore, BS ?? 202-741-2342 ?? fdore@mfa.gwu.edu Less <<
NCT02221180 Bioequivalence Phase 1 Completed - United States, Nebraska ... More >> Lincoln, Nebraska, United States Less <<
NCT03298009 Type2 Diabetes ... More >> Heart Failure Less << Not Applicable Withdrawn(end of contract nego... More >>ciations) Less << January 1, 2019 -
NCT02139943 Diabetes Mellitus, Type 1 Phase 2 Completed - -
NCT01428284 Healthy Phase 1 Completed - United States, Kansas ... More >> Overland Park, Kansas, United States Less <<
NCT02073227 Healthy Volunteers Phase 1 Completed - United States, Arizona ... More >> Tempe, Arizona, United States Less <<
NCT01707316 Healthy Phase 1 Completed - China ... More >> Beijing, China Less <<
NCT02243202 - Completed - -
NCT03436693 Diabetic Nephropathy Phase 3 Recruiting September 2021 Japan ... More >> Research site Recruiting Aichi, Japan Research site Recruiting Chiba, Japan Research site Recruiting Fukuoka, Japan Research site Recruiting Fukushima, Japan Research site Recruiting Gunma, Japan Research site Recruiting Hiroshima, Japan Research site Recruiting Hokkaido, Japan Research site Recruiting Hyogo, Japan Research site Recruiting Ibaraki, Japan Research site Recruiting Kagawa, Japan Research site Recruiting Kagoshima, Japan Research site Recruiting Kanagawa, Japan Research site Recruiting Kumamoto, Japan Research site Recruiting Mie, Japan Research site Recruiting Nagano, Japan Research site Recruiting Nagasaki, Japan Research site Recruiting Oita, Japan Research site Recruiting Okinawa, Japan Research site Recruiting Osaka, Japan Research site Recruiting Saitama, Japan Research site Recruiting Shizuoka, Japan Research site Recruiting Tochigi, Japan Research site Recruiting Tokyo, Japan Research site Recruiting Wakayama, Japan Research site Recruiting Yamagata, Japan Research site Recruiting Yamaguchi, Japan Less <<
NCT02220218 Healthy Phase 1 Completed - United States, Nebraska ... More >> Lincoln, Nebraska, United States Less <<
NCT02597309 Diabetes, Obesity PHASE4 WITHDRAWN 2025-07-17 Joslin Diabetes Center, Boston... More >>, Massachusetts, 02215, United States Less <<
NCT02324842 Type 2 Diabetes Mellitus Not Applicable Recruiting December 2018 United States, Texas ... More >> University of Texas Health Science Center at San Antonio Recruiting San Antonio, Texas, United States, 78229 Contact: Ralph A DeFronzo, MD ?? 210-567-6691 ?? defronzo@uthscsa.edu ?? Contact: Monica Palomo, BS ?? 210-567-6710 ?? palomom@uthscsa.edu ?? Principal Investigator: Ralph A DeFronzo, MD Less <<
NCT01186588 Healthy|Hepatic Insufficiency PHASE1 COMPLETED 2025-04-11 Orlando, Florida, United State... More >>s|Knoxville, Tennessee, United States Less <<
NCT01877889 Healthy Phase 1 Completed - Germany ... More >> Neuss, Germany Less <<
NCT03604224 - Recruiting March 29, 2019 India ... More >> Diacon Hospital Recruiting Bangalore, India, 560010 Dr. A. Ramachandran's Diabetes Hospitals Not yet recruiting Chennai, India, 600032 CARE Hospitals Not yet recruiting Hydrabad, India, 500001 Less <<
NCT02624908 Diabetes Mellitus, Type 2 Phase 4 Recruiting November 2018 United States, Georgia ... More >> Atlanta VA Medical Center Recruiting Decatur, Georgia, United States, 30033 Less <<
NCT01718652 Healthy Phase 1 Completed - Belgium ... More >> Antwerpen, Belgium Less <<
NCT03190798 Type2 Diabetes Mellitus ... More >> Cardiovascular Diseases Less << Phase 4 Withdrawn(Study has been withd... More >>rawn from IRB review pending IND revision) Less << August 1, 2018 United States, Texas ... More >> The University of Texas Health Science Center at San Antonio San Antonio, Texas, United States, 78229 Less <<
NCT02891954 Diabetes Mellitus, Type 2 PHASE1 ACTIVE_NOT_RECRUITING 2025-09-25 -
NCT02673138 Type 1 Diabetes Not Applicable Completed - United States, Connecticut ... More >> Yale University School of Medicine New Haven, Connecticut, United States, 06520 Less <<
NCT02673138 - Completed - -
NCT02000700 Diabetes Mellitus, Type 2 Phase 1 Completed - United States, Arkansas ... More >> Little Rock, Arkansas, United States United States, California Los Angeles, California, United States United States, Colorado Aurora, Colorado, United States United States, Connecticut New Haven, Connecticut, United States United States, Florida Jacksonville, Florida, United States United States, Indiana Indianapolis, Indiana, United States United States, Kansas Lenexa, Kansas, United States United States, Maryland Baltimore, Maryland, United States United States, Missouri Kansas City, Missouri, United States United States, Ohio Toledo, Ohio, United States United States, Pennsylvania Pittsburgh, Pennsylvania, United States United States, Texas Houston, Texas, United States United States, Utah Salt Lake City, Utah, United States Brazil Campinas, Brazil Curitiba, Brazil Ribeir?o Preto, Brazil Sao Paulo, Brazil Less <<
NCT01157000 Healthy PHASE1 COMPLETED 2025-06-10 Merksem, Belgium
NCT02912455 Diabetes Mellitus, Type 2 ... More >> Obesity Less << Phase 4 Recruiting July 31, 2018 United States, Ohio ... More >> Cleveland Clinic Recruiting Cleveland, Ohio, United States, 44195 Contact: Sangeeta Kashyap, MD ?? 216-445-2679 ?? kashyas@ccf.org ?? Contact: Mario Scarcipino ?? 216-444-3599 ?? mascar@ccf.org ?? Principal Investigator: Sangeeta Kashyap, MD Less <<

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Preparing Stock Solutions 1mg 5mg 10mg

1 mM

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2.25mL

0.45mL

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11.25mL

2.25mL

1.12mL

22.50mL

4.50mL

2.25mL

 

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