Pioglitazone HCl

別名: AD-4833, U-72107E 中文名稱：鹽酸吡格列酮

目錄號(hào)：S2046 Purity: 99.88%

Pioglitazone HCl (AD-4833, U-72107E) 是一種 cytochrome P450 (CYP)2C8 和 CYP3A4 酶的抑制劑。Pioglitazone HCl 抑制CYP2C8、CYP3A4和CYP2C9的Ki值分別為1.7 μM、11.8 μM和32.1 μM。Pioglitazone HCl 也是一種選擇性的 peroxisome proliferator-activated receptor-gamma (PPARγ) 激動(dòng)劑，對(duì)人PPARγ和小鼠PPARγ的EC50值分別為0.93 μM和0.99 μM。Pioglitazone HCl 可抑制線粒體內(nèi)鐵的攝取、脂質(zhì)過(guò)氧化和隨后的鐵死亡。

Pioglitazone HCl Chemical Structure

CAS: 112529-15-4

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	790	現(xiàn)貨
10mg	647.01	現(xiàn)貨
50mg	1387.89	現(xiàn)貨
200mg	3019.29	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.88%

99.88

Pioglitazone HCl相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	P450 CYP2 CYP51 CYP3 CYP735 CYP11 CYP26 CYP2C9 CYP1 CYP17	點(diǎn)擊展開(kāi)
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細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
HEK293T	Function assay	1 uM	24 hrs	Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 1 uM after 24 hrs by luciferase reporter gene assay	21030263
HEK293	Function assay	10 uM	24 hrs	Transactivation of PPAR-gamma (unknown origin) expressed in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay	24890090
THP1	Function assay	10 uM	24 hrs	Upregulation of ABCA1 mRNA expression in human THP1 cells at 10 uM after 24 hrs by qPCR method relative to control	27220065
THP1	Function assay	10 uM	24 hrs	Upregulation of ABCG1 mRNA expression in human THP1 cells at 10 uM after 24 hrs by qPCR method relative to control	27220065
PC3	Function assay	50 uM	24 hrs	Increase in p21(WAF1) protein expression in human PC3 cells at 50 uM incubated for 24 hrs by Western blot analysis	28395220
MDA-MB-231	Function assay	50 uM	24 hrs	Increase in p21(WAF1) protein expression in human MDA-MB-231 cells at 50 uM incubated for 24 hrs by Western blot analysis	28395220
SCC15	Cytotoxicity assay	50 uM	24 hrs	Cytotoxicity against human SCC15 cells transfected with PPARalpha siRNA assessed as reduction in cell viability at 50 uM after 24 hrs by resazurin reduction assay	29031063
SCC15	Cytotoxicity assay	50 uM	24 hrs	Cytotoxicity against human SCC15 cells transfected with PPARbeta siRNA assessed as reduction in cell viability at 50 uM after 24 hrs by resazurin reduction assay	29031063
3T3L1	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in AP1 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	30594432
3T3L1	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in CD36 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	30594432
3T3L1	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in Glut4 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	30594432
3T3L1	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in adiponectin mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	30594432
K562	Function assay	10 uM	72 hrs	Induction of sensitization to imatinib-induced cytotoxicity in imatinib-resistant human K562-IMA[r] cells assessed as induction of cell death at 10 uM after 72 hrs in presence of 1 uM imatinib by propidium iodide/Triton-X100 dye based FACS analysis	31648125
3T3L1	Function assay	100 umol/L		Increase in PPARgamma mRNA levels in mouse 3T3L1 cells at 100 umol/L by RT-PCR	20392645
HepG2	Function assay	30 uM		Binding affinity to NAF1 (unknown origin) expressed in human HepG2 cells assessed as inhibition of mitochondrial respiration at 30 uM	30770154
HepG2	Function assay	30 uM		Binding affinity to NAF1 in human HepG2 cells assessed as inhibition of mitochondrial respiration at 30 uM	30770154
Cos7	Function assay		14 hrs	Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay, EC50=0.3μM.	20307981
CHO	Function assay		24 hrs	Partial agonist activity at human PPARgamma expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay, EC50=0.39μM.	21377875
HepG2	Function assay		20 hrs	Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay, EC50=0.57μM.	22341573
HEK293	Function assay		18 hrs	Transactivation of human GAL4-fused PPARgamma ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay, EC50=0.8μM.	23102891
THP1	Antiinflammatory assay		1 hr	Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA, IC50=18.84μM.	23811092
THP1	Antiinflammatory assay		2 hrs	Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion incubated for 2 hrs prior to PMA challenge measured after 72 hrs by ELISA, IC50=18.6μM.	24531227
HEK293	Function assay		18 hrs	Agonist activity at human PPARgamma expressed in HEK293 cells incubated for 18 hrs by luciferase reporter gene assay, EC50=0.21μM.	25333853
COS7	Function assay		42 hrs	Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay, EC50=0.5μM.	27560282
COS7	Function assay		42 hrs	Transactivation at Gal4 fused PPARgamma LBD (unknown origin) expressed in African green monkey COS7 cells after 42 hrs by luciferase assay, EC50=0.32μM.	27569195
COS7	Function assay		42 hrs	Transactivation of Gal4 fused human PPARgamma LBD expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay, EC50=0.38μM.	27918994
HEK293	Function assay		24 hrs	Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50=1.1μM.	28465099
HEK293	Function assay		4 hrs	Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreated for 4 hrs followed by TNFalpha stimulation after 3 hrs by luciferase reporter gene assay, IC50=22μM.	28465099
HepG2	Function assay		24 hrs	Agonist activity at PPARgamma in human HepG2 cells assessed as activation of PPRE incubated for 24 hrs by dual luciferase reporter gene assay, EC50=0.24μM.	30001846
HEK293BENA	Function assay		24 hrs	Transactivation of GAL4-fused human PPARgamma transfected in HEK293BENA cells after 24 hrs by steady glo-luciferase reporter gene assay, EC50=2.053μM.	30351933
HEK293	Function assay		18 hrs	Transactivation of human full length PPARgamma expressed in HEK293 cells after 18 hrs by luciferase reporter gene based luminescence assay, EC50=0.1μM.	30362739
293H	Function assay		16 hrs	Transactivation of GAL4-DBD fused human PPARgamma ligand binding domain expressed in UAS-bla HEL 293H cells preincubated for 16 hrs followed by FRET substrate addition and measured after 2 hrs by TR-FRET assay, EC50=0.098μM.	30429097
stem cells	Function assay		5 days	Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as increase in adiponectin production measured on day 5 in presence of IDX by ELISA, EC50=0.35μM.	30672698
HEK293T	Function assay		18 hrs	Transactivation of full length human PPARgamma2 expressed in HEK293T cells co-expressing PPRE after 18 hrs by luciferase reporter gene assay, EC50=0.25μM.	30676741
HEK293T	Function assay		18 hrs	Transactivation of chimeric Gal4 yeast DBD fused-PPARgamma LBD (unknown origin) expressed in HEK293T cells co-expressing PPRE after 18 hrs by luciferase reporter gene assay, EC50=0.35μM.	30676741
COS7	Function assay		39 hrs	Transactivation of Gal4-fused human PPARgamma transfected in COS7 cells co-transfected with pGAL5-TK-pGL3 and pRennilla-CMV incubated for 39 hrs by dual luciferase reporter assay, EC50=1.4μM.	31648125
HepG2 cells	Function assay			Peroxisome proliferator activated receptor gamma agonistic activity in HepG2 cells, EC50=7.6 μM	10714503
COS cells	Function assay			Transcriptional activation in COS cells expressing PPAR gamma and RXR alpha; values in the parentheses indicates 95% confidence interval, EC50=0.49 μM	11906293
CV-1	Function assay			In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells, EC50=0.69μM.	8576907
3T3-L1	Function assay			Effective concentration for 50% enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells, EC50=0.16μM.	9599241
CV-1	Function assay			Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells, EC50=0.58884μM.	9836620
CV-1	Function assay			Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay, EC50=0.58μM.	11720854
HEK293	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with steroid receptor coactivator-1 by EYFP based reporter gene assay	16680159
HEK293	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with retinoid X-receptor alpha by EYFP based reporter gene assay	16680159
CV1	Function assay			Transactivation of PPARgamma in CV1 cells, EC50=0.55μM.	16821769
CHO	Function assay			Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay, EC50=0.14μM.	20656494
COS-1	Function assay			Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay, EC50=0.39μM.	21130649
COS7	Function assay			Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay, EC50=0.3μM.	21873070
Sf21	Function assay			Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50=0.3μM.	21965623
Sf21	Function assay			Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50=2μM.	21965623
COS7	Function assay			Transactivation of GAL4-fused human PPARgamma ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay, EC50=0.2μM.	23130964
COS7	Function assay			Transactivation of human PPARgamma expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay, EC50=0.2μM.	26595749
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

Ferroptosis ^[8]	hPPARγ ^[1] (Cell-free assay)	rPPARγ ^[6] (Cell-free assay)	CYP2C8 ^[7] (Cell-free assay)	CYP3A4 ^[7] (Cell-free assay)	點(diǎn)擊更多
	0.93 μM(EC50)	0.99 μM(EC50)	1.7 μM(Ki)	11.8 μM(Ki)	點(diǎn)擊更多

體外研究(In Vitro)
體外研究活性	Pioglitazone抑制LPS誘導(dǎo)的iNOS表達(dá)和NO的產(chǎn)生，并抑制iNOS表達(dá)足以保護(hù)多巴胺神經(jīng)元抗LPS損傷。Pioglitazone保護(hù)多巴胺能神經(jīng)元免受LPS，至少通過(guò)抑制iNOS的表達(dá)和NO的產(chǎn)生，這是通過(guò)抑制p38蛋白激酶的活性介導(dǎo)的。Pioglitazone抑制p38蛋白的LPS誘導(dǎo)的磷酸化。^[1]

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在雄性肥胖鼠中，Pioglitazone口服（0.3-3毫克/公斤/天7天）劑量依賴性地降低了高血糖癥，高脂血癥，和高胰島素血癥。在大鼠中，Pioglitazone改善葡萄糖耐受性和增加外源性胰島素和血漿甘油三酯的清除。^[2] 在未處理的SOD1-G93A小鼠中，Pioglitazone處理轉(zhuǎn)基因小鼠顯示改進(jìn)的肌肉力量和體重，表現(xiàn)出延遲疾病發(fā)作和顯著較長(zhǎng)生存比。^[3] 在大鼠和小鼠中，Pioglitazone顯著降低高血糖癥，高脂血癥，高胰島素血癥，葡萄糖不耐癥，其特征如胰島素抵抗?fàn)顟B(tài)。在黃色的KK小鼠的隔膜和脂肪組織中，Pioglitazone在的胰島素介導(dǎo)的葡萄糖代謝。在Zucker肥胖大鼠中，Pioglitazone增強(qiáng)在源性胰島素的血糖反應(yīng)。^[4] 在APPV717I轉(zhuǎn)基因小鼠的海馬和皮層活性星形細(xì)胞中，Pioglitazone導(dǎo)致激活的小膠質(zhì)細(xì)胞的數(shù)量減少。在APPV717I轉(zhuǎn)基因小鼠中，Pioglitazone降低β-分泌-1（BACE1）的mRNA和蛋白水平。^[5]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05946564	Not yet recruiting	ANCA Associated Vasculitis\|Rapidly Progressive Glomerulonephritis\|Crescentic Glomerulonephritis	Assistance Publique - H?pitaux de Paris\|Ministry of Health France	July 2023	Phase 3
NCT05305287	Recruiting	Non-Alcoholic Fatty Liver Disease\|Type 2 Diabetes\|Mitochondrial Metabolism Disorders	The University of Texas Health Science Center at San Antonio\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	November 1 2022	Phase 4
NCT05411965	Completed	Diabetes Mellitus Type 2	Boryung Pharmaceutical Co. Ltd	April 28 2022	Phase 1
NCT04501406	Recruiting	Type 2 Diabetes Mellitus (T2DM)\|Nonalcoholic Steatohepatitis	University of Florida\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	December 15 2020	Phase 2
NCT04535700	Completed	Type 2 Diabetes	Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal	September 18 2020	Phase 4
NCT00904046	Recruiting	Uric Acid Kidney Stone Disease	University of Texas Southwestern Medical Center\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)\|Takeda Pharmaceuticals North America Inc.	September 5 2019	Not Applicable

參考文獻(xiàn)
[1] Xing B, et al. J Neuroinflammation,?008, 5, 4. [2] Sugiyama Y, et al. Arzneimittelforschung,?990, 40(3), 263-267. [3] Burkhard Schütz, et al. J Neurosci,?005, 25(34), 7805-7812. [4] Ikeda H, et al. Arzneimittelforschung,?990, 40(2 Pt 1), 156-162. [5] Kondo T, et al. Arzneimittelforschung,?996, 46(6), 594-600. [6] Kenji Kuwabara, et al. J Pharmacol Exp Ther . 2004 Jun;309(3):970-7. [7] Jasminder Sahi, et al. Drug Metab Dispos . 2003 Apr;31(4):439-46. [8] Hua Yuan, et al. Biochem Biophys Res Commun . 2016 Sep 16;478(2):838-44. + 展開(kāi)

參考文獻(xiàn)

[1] Xing B, et al. J Neuroinflammation,?008, 5, 4.
[2] Sugiyama Y, et al. Arzneimittelforschung,?990, 40(3), 263-267.
[3] Burkhard Schütz, et al. J Neurosci,?005, 25(34), 7805-7812.

[4] Ikeda H, et al. Arzneimittelforschung,?990, 40(2 Pt 1), 156-162.
[5] Kondo T, et al. Arzneimittelforschung,?996, 46(6), 594-600.
[6] Kenji Kuwabara, et al. J Pharmacol Exp Ther . 2004 Jun;309(3):970-7.
[7] Jasminder Sahi, et al. Drug Metab Dispos . 2003 Apr;31(4):439-46.
[8] Hua Yuan, et al. Biochem Biophys Res Commun . 2016 Sep 16;478(2):838-44.

+ 展開(kāi)

化學(xué)信息&溶解度

分子量	392.9	分子式	C₁₉H₂₀N₂O₃S.HCl
CAS號(hào)	112529-15-4	SDF	Download Pioglitazone HCl SDF
Smiles	CCC1=CN=C(C=C1)CCOC2=CC=C(C=C2)CC3C(=O)NC(=O)S3.Cl
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 79 mg/mL ( (201.06 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 4 mg/mL (10.18 mM)

Water : Insoluble

DMSO : 78 mg/mL ( (198.52 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 4 mg/mL (10.18 mM)

Water : Insoluble

DMSO : 78 mg/mL ( (198.52 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 4 mg/mL (10.18 mM)

Water : Insoluble

DMSO : 79 mg/mL ( (201.06 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 7 mg/mL (17.81 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度批次：現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑					動(dòng)物體內(nèi)配方計(jì)算器
	澄清溶液	5%DMSO 1 Corn oil	5.0mg/ml (12.73mM)	以 1 mL 工作液為例，取50μL100mg/ml的澄清DMSO儲(chǔ)備液加到950μL玉米油中，混合均勻。工作液請(qǐng)現(xiàn)配現(xiàn)用！	動(dòng)物體內(nèi)配方計(jì)算器
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml (12.73mM)	以 1 mL 工作液為例,取50μL100mg/ml的澄清DMSO儲(chǔ)備液加到400μLPEG300中,混合均勻使其澄清;向上述體系中加入50μLTween80,混合均勻使其澄清;然后繼續(xù)加入500μLddH2O定容至1mL。工作液請(qǐng)現(xiàn)配現(xiàn)用!
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.0mg/ml (5.09mM)	以 1 mL 工作液為例，取50μL40mg/ml的澄清DMSO儲(chǔ)備液加到400μL PEG300中，混合均勻使其澄清；向上述體系中加入50μLTween80，混合均勻使其澄清；然后繼續(xù)加入500μL ddH2O定容至 1 mL。工作液請(qǐng)現(xiàn)配現(xiàn)用！

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術(shù)支持

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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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