CMPD101 - ≥98%(HPLC), high purity , CAS No.865608-11-3, Inhibitor of beta adrenergic receptor kinase 1;Inhibitor of beta adrenergic receptor kinase 2

Item Number

C287795

Grouped product items
SKU	Size	Availability	Price
C287795-5mg	5mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$157.90
C287795-10mg	10mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$252.90
C287795-25mg	25mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$569.90
C287795-50mg	50mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$886.90

Potent and selective GRK2/3 inhibitor

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Basic Description

Synonyms	3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide；3-(((4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)methyl)amino)-N-(2-(trifluoromethyl)benzyl)benzamide
Specifications & Purity	Moligand™, ≥98%(HPLC)
Biochemical and Physiological Mechanisms	Potent and selective GRK2/3 inhibitor (IC50values are 32 and 54 nM for GRK3 and GRK2, respectively). Exhibits selectivity for GRK2/3 over GRK1/5. ReducesDAMGO-induced desensitization and internalization ofμ-opioid receptors.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of beta adrenergic receptor kinase 1;Inhibitor of beta adrenergic receptor kinase 2
Product Description	product description： CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure。

Names and Identifiers

IUPAC Name	3-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide
INCHI	InChI=1S/C24H21F3N6O/c1-33-21(31-32-22(33)16-9-11-28-12-10-16)15-29-19-7-4-6-17(13-19)23(34)30-14-18-5-2-3-8-20(18)24(25,26)27/h2-13,29H,14-15H2,1H3,(H,30,34)
InChi Key	WFOVEDJTASPCIR-UHFFFAOYSA-N
Canonical SMILES	CN1C(=NN=C1C2=CC=NC=C2)CNC3=CC=CC(=C3)C(=O)NCC4=CC=CC=C4C(F)(F)F
Isomeric SMILES	CN1C(=NN=C1C2=CC=NC=C2)CNC3=CC=CC(=C3)C(=O)NCC4=CC=CC=C4C(F)(F)F
PubChem CID	11677079
MeSH Entry Terms	3-((4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino)-N-((2-(trifluoromethyl)phenyl)methyl)benzamide;CMPD101
Molecular Weight	466.46

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4 results found

Lot Number	Certificate Type	Date	Item
D23141394	Certificate of Analysis	Mar 06, 2023	C287795
D23141395	Certificate of Analysis	Mar 06, 2023	C287795
D23141396	Certificate of Analysis	Mar 06, 2023	C287795
D23141398	Certificate of Analysis	Mar 06, 2023	C287795

References

1. Thal DM, Yeow RY, Schoenau C, Huber J, Tesmer JJ. (2011) Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors.. Mol Pharmacol, 80 (2): (294-303). [PMID:21596927]
2. Lowe JD, Sanderson HS, Cooke AE, Ostovar M, Tsisanova E, Withey SL, Chavkin C, Husbands SM, Kelly E, Henderson G et al.. (2015) Role of G Protein-Coupled Receptor Kinases 2 and 3 in μ-Opioid Receptor Desensitization and Internalization.. Mol Pharmacol, 88 (2): (347-56). [PMID:26013542]

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Basic Description