Product Name :
TGFβRI-IN-2
Description:
TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.
CAS:
1976038-41-1
Molecular Weight:
411.82
Formula:
C20H15ClFN5O2
Chemical Name:
2-1-[2-(5-chloro-2-fluorophenyl)-5-methylpyridin-4-yl]-2-oxo-1H,2H,3H-imidazo[4,5-c]pyridin-3-ylacetamide
Smiles :
CC1=CN=C(C=C1N1C2C=CN=CC=2N(CC(N)=O)C1=O)C1=CC(Cl)=CC=C1F
InChiKey:
LVEUPFUJRKZPEN-UHFFFAOYSA-N
InChi :
InChI=1S/C20H15ClFN5O2/c1-11-8-25-15(13-6-12(21)2-3-14(13)22)7-17(11)27-16-4-5-24-9-18(16)26(20(27)29)10-19(23)28/h2-9H,10H2,1H3,(H2,23,28)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.|Product information|CAS Number: 1976038-41-1|Molecular Weight: 411.82|Formula: C20H15ClFN5O2|Chemical Name: 2-1-[2-(5-chloro-2-fluorophenyl)-5-methylpyridin-4-yl]-2-oxo-1H,2H,3H-imidazo[4,5-c]pyridin-3-ylacetamide|Smiles: CC1=CN=C(C=C1N1C2C=CN=CC=2N(CC(N)=O)C1=O)C1=CC(Cl)=CC=C1F|InChiKey: LVEUPFUJRKZPEN-UHFFFAOYSA-N|InChi: InChI=1S/C20H15ClFN5O2/c1-11-8-25-15(13-6-12(21)2-3-14(13)22)7-17(11)27-16-4-5-24-9-18(16)26(20(27)29)10-19(23)28/h2-9H,10H2,1H3,(H2,23,28)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.DREADD agonist 21 manufacturer |Shelf Life: ≥12 months if stored properly.[Leu5]-Enkephalin Neuronal Signaling |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:33107782 |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|TGFβRI-IN-2 (compound 18) at 1 μM shows a 31% inhibition of MAP3K2 (MEKK2) with an IC50 value of 2.2 μM.|In Vivo:|TGFβRI-IN-2 (oral administation; 50, 150 and 500 mg/kg; 5 days) induces cardiovascular toxicity characterized by valvular interstitial cell proliferation, neutrophil presence, hemorrhage and fibrin deposition in the heart valves.|References:|Wang H, et al. Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors.Bioorg Med Chem Lett. 2016 Sep 1;26(17):4334-9.Products are for research use only. Not for human use.|