Identification | Back Directory | [Name]
YC-1 | [CAS]
170632-47-0 | [Synonyms]
YC-1 CS-2261 Nsc728165 LIFICIGUAT YC-1(Lificiguat) Lificiguat(YC-1) YC 1 (pharMaceutical) YC-1 - CAS 170632-47-0 - Calbiochem 1-benzyl-3-(5-hydroxymethyl-2-furyl)indazole 1-Benzyl-3-(5-hydroxymethylfur-2-yl)indazole 3-(5'-HYDROXYMETHYL-2'-FURYL)-1-BENZYLINDAZOLE 1-benzyl-3-(5-hydroxymethyl-furan-2-yl)indazole (5-(1-Benzyl-1H-indazol-3-yl)furan-2-yl)Methanol 5-[1-(PHENYLMETHYL)-1H-INDAZOL-3-YL]-2-FURANMETHANOL 2-Furanmethanol, 5-[1-(phenylmethyl)-1H-indazol-3-yl]- YC-1 (3-(5'-HYDROXYMETHYL-2'-FURYL)-1-BE NZYL INDAZOLE) \ GUANYLYL CYCLASE ACTI | [Molecular Formula]
C19H16N2O2 | [MDL Number]
MFCD06407798 | [MOL File]
170632-47-0.mol | [Molecular Weight]
304.34 |
Chemical Properties | Back Directory | [Melting point ]
110-112℃ | [Boiling point ]
522.2±50.0 °C(Predicted) | [density ]
1.24±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Room Temperature | [solubility ]
DMSO: 12 mg/mL
| [form ]
solid
| [pka]
13.83±0.10(Predicted) | [color ]
white
| [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
Hazard Information | Back Directory | [Description]
YC-1 (170632-47-0) is a nitric oxide-independent activator of soluble guanylyl cyclase (sGC). Significantly elevates cGMP levels and inhibits collagen-stimulated aggregation of rabbit platelets (IC50?= 14.6 μM).1?Induces human endometrial cancer cell senescence via modulation of HIF1α activity.2?Induces degradation of HIF1α.3?Protects against glutamate-induced neuronal damage4?and β-amyloid-induced toxicity in differentiated PC12 cells5. | [Uses]
YC-1 has been used as a hypoxia-inducible factor 1α (HIF-1α) inhibitor:
- to reduce hypoxia induced Jagged1 expression in cardiomyocytes (CMs)
- to study its effect on progenitor expansion and CD34+ and side population (SP) cell phenotype and on the proliferation rate of cells with an ability to form long term colony forming units
- to study its effect on regulating sphingosine 1-phosphate (S1P) bound to albumin induced plasminogen activator inhibitor 1 (PAI-1) expression by activating Rho/ Rho-associated protein kinase (ROCK) pathway.
| [Definition]
ChEBI: Lificiguat is a member of the class of indazoles that is 1H-indazole which is substituted by a benzyl group at position 1 and a 5-(hydroxymethyl)-2-furyl group at position 3. It is an activator of soluble guanylate cyclase and inhibits platelet aggregation. It has a role as an antineoplastic agent, a soluble guanylate cyclase activator, an apoptosis inducer, a platelet aggregation inhibitor and a vasodilator agent. It is a member of indazoles, a member of furans and an aromatic primary alcohol. | [General Description]
A nitric oxide-independent, superoxide-sensitive activator of soluble guanylyl cyclase. Inhibits platelet adhesion to collagen and acts as an antithrombotic agent. Reported to reduce HIF-1α levels and xenograft growth. | [Biochem/physiol Actions]
YC-1 activates soluble guanylyl cyclase and prevents platelet aggregation and vascular contraction. It has a potential to treat circulation disorders. YC-1 also has an ability to inhibit hypoxia-inducible factor 1α (HIF-1α) activity in vitro. It acts as a potential antiangiogenic anticancer agent. | [storage]
+4°C | [References]
1) Martin?et al.?(2001),?YC-1 activation of human soluble guanylyl cyclase has both heme-dependent and heme-independent components;?Proc. Natl. Acad. Sci. USA,?98?12938
2) Kato?et al.?(2006),?Induction of human endometrial cancer cell senescence through modulation of HIF-1alpha activity by EGLN1; Int. J. Cancer,?118?1144
3) Kim?et al.?(2006),?A domain responsible for HIF-1alpha degradation by YC-1, a novel anticancer agent; Int. J. Oncol.,?29?255
4) Tai?et al. (2018),?Therapeutic window for YC-1 following glutamate-induced neuronal damage and transient focal cerebral ischemia; Mol. Med. Rep.,?17?6490
5) Tsai?et al.?(2013),?The role of heat shock protein 70 in the protective effect of YC-1 on β-amyloid-induced toxicity in differentiated PC12 cells.; PLoS One,?8(7)?e69320 |
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Company Name: |
LGM Pharma
|
Tel: |
1-(800)-881-8210 |
Website: |
www.lgmpharma.com |
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