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PARP&Proteasome

Grapiprant (415903-37-6)

Grapiprant, also known as AT-001 and CJ-023, is a drug from the piprant class. These molecules were derived from acylsulfonamide and are characterized to be a novel series of para-N-acylaminomethylbenzoic acid known to be prostaglandin receptor antagonists.

Not Intended for Therapeutic Use. For research use only.

CAS: 415903-37-6 Category

Grapiprant (415903-37-6) Description:

Grapiprant, also known as CJ-023,423, RQ-00000007 and AAT-007, is a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties. It is currently under development for use in humans and dogs for the control of pain and inflammation associated with osteoarthritis.

In vitro, CJ-023,423 inhibits [(3)H]PGE(2) binding to both human and rat EP(4) receptors with K(i) of 13 +/- 4 and 20 +/- 1 nM, respectively. CJ-023,423 is highly selective for the human EP(4) receptor over other human prostanoid receptor subtypes. It also inhibits PGE(2)-evoked elevation in intracellular cAMP at the human and rat EP(4) receptors with pA(2) of 8.3 +/- 0.03 and 8.2 +/- 0.2 nM, respectively. In vivo, oral administration of CJ-023,423 significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE(2) (ED(50) = 12.8 mg/kg).

Grapiprant (415903-37-6) Specifications:

Product Name Grapiprant
Synonyms CJ-023423;CJ023423;AAT-007;AAT007;AAT 007; RQ-00000007; RQ 00000007; RQ00000007;
Chemical Name N-((4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenethyl)carbamoyl)-4-methylbenzenesulfonamide;1-(2-(4-(2-ethyl-4,6-dimethylimidazo(4,5-c)pyridin-1-yl)phenyl)ethyl)-3-(4-methylphenyl)sulfonylurea
Purity ≥98%
CAS Number 415903-37-6
Molecular Formula C26H29N5O3S
Molecular Weight 491.60516
Monoisotopic Mass 491.199 g/mol
MDL number N/A
InChIKey HZVLFTCYCLXTGV-UHFFFAOYSA-N
InChi Code InChI=1S/C26H29N5O3S/c1-5-24-29-25-19(4)28-18(3)16-23(25)31(24)21-10-8-20(9-11-21)14-15-27-26(32)30-35(33,34)22-12-6-17(2)7-13-22/h6-13,16H,5,14-15H2,1-4H3,(H2,27,30,32)
SMILES O=C(NCCC1=CC=C(C=C1)N2C(CC)=NC3=C(N=C(C=C32)C)C)NS(C4=CC=C(C=C4)C)(=O)=O
Form Powder
Color N/A
Solubility  Soluble in DMSO, not in water
Storage Temp.  -20°C
Shelf life ≥ 2 years
Handling Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Provide appropriate exhaust ventilation at places where dust is formed
Application It is currently under development for use in humans and dogs for the control of pain and inflammation associated with osteoarthritis.

 


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