MedKoo Cat#: 526748 | Name: GSK466317A

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK466317A is a GRK2 inhibitor. GRK2 has been directly implicated in the progression of heart failure. Selective inhibitors of individual subfamilies of G protein-coupled receptor kinases (GRKs) would serve as useful chemical probes as well as leads for therapeutic applications ranging from heart failure to Parkinson's disease.

Chemical Structure

GSK466317A
GSK466317A
CAS#864082-48-4

Theoretical Analysis

MedKoo Cat#: 526748

Name: GSK466317A

CAS#: 864082-48-4

Chemical Formula: C21H16ClF3N4O2

Exact Mass: 448.0914

Molecular Weight: 448.83

Elemental Analysis: C, 56.20; H, 3.59; Cl, 7.90; F, 12.70; N, 12.48; O, 7.13

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
GSK466317A; GSK-466317A; GSK 466317A.
IUPAC/Chemical Name
N-(7-chloro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide
InChi Key
OYNBTBJATZVIGH-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H16ClF3N4O2/c1-10-18(20(31)28-14-6-12-9-26-29-19(12)16(22)7-14)15(8-17(30)27-10)11-2-4-13(5-3-11)21(23,24)25/h2-7,9,15H,8H2,1H3,(H,26,29)(H,27,30)(H,28,31)
SMILES Code
O=C(C1=C(C)NC(CC1C2=CC=C(C(F)(F)F)C=C2)=O)NC3=CC4=C(NN=C4)C(Cl)=C3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 448.83 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1. Identification and Structure-​Function Analysis of Subfamily Selective G Protein-​Coupled Receptor Kinase Inhibitors. By Homan, Kristoff T.; Larimore, Kelly M.; Elkins, Jonathan M.; Szklarz, Marta; Knapp, Stefan; Tesmer, John J. G. From ACS Chemical Biology (2015), 10(1), 310-319. 2. Development of Dihydropyridone Indazole Amides as Selective Rho-​Kinase Inhibitors. By Goodman, Krista B.; Cui, Haifeng; Dowdell, Sarah E.; Gaitanopoulos, Dimitri E.; Ivy, Robert L.; Sehon, Clark A.; Stavenger, Robert A.; Wang, Gren Z.; Viet, Andrew Q.; Xu, Weiwei; et al. From Journal of Medicinal Chemistry (2007), 50(1), 6-9. 3. Preparation of amido-​substituted indazoles as Rho-​kinase inhibitors. By Lee, Dennis; Goodman, Krista B. From PCT Int. Appl. (2005), WO 2005082890 A1 20050909.