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MedKoo Cat#: 526747 | Name: GSK299115A

Description:

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

GSK299115A is a G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor (GRK2 inhibitor). G-protein-coupled receptor kinase 2 (GRK2) is a G-protein-coupled receptor kinase that is ubiquitously expressed in many tissues and regulates various intracellular mechanisms. GRK2 plays an important role in the maintenance of heart structure and function; thus, this kinase is involved in many cardiovascular diseases.

Chemical Structure

GSK299115A
GSK299115A
CAS#864082-35-9

Theoretical Analysis

MedKoo Cat#: 526747

Name: GSK299115A

CAS#: 864082-35-9

Chemical Formula: C20H16Cl2N4O2

Exact Mass: 414.0650

Molecular Weight: 415.27

Elemental Analysis: C, 57.85; H, 3.88; Cl, 17.07; N, 13.49; O, 7.71

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
GSK299115A; GSK 299115A; GSK-299115A.
IUPAC/Chemical Name
4-(3,4-Dichlorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyridine-5-carboxamide
InChi Key
RHTXWIKPNGROHZ-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H16Cl2N4O2/c1-10-19(20(28)25-13-3-5-17-12(6-13)9-23-26-17)14(8-18(27)24-10)11-2-4-15(21)16(22)7-11/h2-7,9,14H,8H2,1H3,(H,23,26)(H,24,27)(H,25,28)
SMILES Code
O=C(C1=C(C)NC(CC1C2=CC=C(Cl)C(Cl)=C2)=O)NC3=CC4=C(NN=C4)C=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
The up- or down-regulation of GRK2 correlates with several pathological disorders. GRK2 up-regulation can worsen cardiac ischemia; furthermore, increased kinase levels occur during the early stages of heart failure and in hypertensive subjects. GRK2 up-regulation can lead to changes in the insulin signaling cascade, which can translate to insulin resistance. Increased GRK2 levels also correlate with the degree of cognitive impairment that is typically observed in Alzheimer’s disease.

Preparing Stock Solutions

The following data is based on the product molecular weight 415.27 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
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives Manuela Guccione, Roberta Ettari, Sabrina Taliani, Federico Da Settimo, Maria Zappalà, and Silvana Grasso Publication Date (Web): June 30, 2016 (Perspective) DOI: 10.1021/acs.jmedchem.5b01939