ChemicalBook > CAS DataBase List > Grapiprant

Grapiprant

Product Name: Grapiprant
CAS No.: 415903-37-6
Chemical Name: Grapiprant
Synonyms: N-((4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenethyl)carbamoyl)-4-methylbenzenesulfonamide;RQ 7;MR 10A7;AAT 007;CS-1556;Grprant;Grapiron;Graprant;Koplante;CJ-023423
CBNumber: CB03054518
Molecular Formula: C26H29N5O3S
Formula Weight: 491.61
MOL File: 415903-37-6.mol

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Grapiprant Property

Melting point:: >151°C (dec.)
Density: 1.29±0.1 g/cm3(Predicted)
storage temp.: Sealed in dry,Store in freezer, under -20°C
solubility: Soluble in DMSO (up to at least 10 mg/ml)
pka: 5.19±0.10(Predicted)
form: solid
color: Off-white
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChI: 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)
InChIKey: HZVLFTCYCLXTGV-UHFFFAOYSA-N
SMILES: C1(S(NC(NCCC2=CC=C(N3C4C=C(C)N=C(C)C=4N=C3CC)C=C2)=O)(=O)=O)=CC=C(C)C=C1

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H303May be harmfulif swallowed

H320Causes eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 10010355
Product name: CJ-023423
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 10010355
Product name: CJ-023423
Purity: ≥98%
Packaging: 5mg
Price: $100
Updated: 2024/03/01

Cayman Chemical

Product number: 10010355
Product name: CJ-023423
Purity: ≥98%
Packaging: 10mg
Price: $184
Updated: 2024/03/01

Cayman Chemical

Product number: 10010355
Product name: CJ-023423
Purity: ≥98%
Packaging: 25mg
Price: $267
Updated: 2024/03/01

ChemScene

Product number: CS-5392
Product name: Grapiprant
Purity: 99.45%
Packaging: 5mg
Price: $110
Updated: 2021/12/16

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Grapiprant Chemical Properties,Usage,Production

Description

Prostaglandin E₂ (PGE₂) activates four E prostanoid (EP) receptors, EP_1-4. EP₄ is a G_s protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis. CJ-023423 is a potent and selective antagonist of the EP₄ receptor (K_i = 13 and 20 nM for human and rat EP₄, respectively). It inhibits PGE₂-evoked elevation in intracellular cAMP in cells and, in vivo, reduces thermal hyperalgesia induced by intraplantar injection of PGE₂. CJ-023423 reduces acute and chronic inflammatory pain in different mouse models.

Uses

CJ-023423 is a potent and selective antagonist of E prostanoid 4 (EP4) receptor.

Biological Functions

Grapiprant (CJ-023423) is an orally available, a potent and selective EP4 receptor antagonist that exhibits significant inhibitory effects on paw swelling, inflammatory biomarkers, synovial inflammation and bone destruction in AIA rats. Grapiprant is highly selective for the human EP4 receptor over other human prostanoid receptor subtypes. It also inhibits PGE2-evoked elevation in intracellular cAMP at the human and rat EP4 receptors with pA2 of 8.3 and 8.2 nM, respectively. In vivo, oral administration of grapiprant significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE2 (ED50 = 12.8 mg/kg). It is also effective in models of acute and chronic inflammatory pain. Grapiprant significantly reduces mechanical hyperalgesia in the carrageenan model. Furthermore, it significantly reverses complete Freund′s adjuvant-induced chronic inflammatory pain response. It produces antihyperalgesic effects in animal models of inflammatory pain. Grapiprant is approved and widely used for treatment of osteoarthritis related pain in dogs. Grapiprant is classify as a non-cyclooxygenase inhibiting non-steroidal anti-inflammatory drug (NSAID).

Side effects

Possible side effects of Grapiprant include: vomiting, drowsiness, diarrhoea, loss of appetite, blood or mucus in the stool, and reduced blood protein levels. The degree of reaction can vary from mild to severe, but if your dog experiences a loss of appetite or abnormal faeces, you should contact your veterinarian promptly.

in vitro

in vitro, cj-023,423 was able to inhibit [(3)h]pge(2) binding to both human and rat ep(4) receptors. cj-023,423 was found to be highly selective for the human ep(4) receptor over other human prostanoid receptor subtypes. cj-023,423 also inhibited pge(2)-evoked elevation in intracellular camp at the human and rat ep(4) receptors with pa(2) of 8.3 and 8.2 nm, respectively [1].

in vivo

in vivo, po administration of cj-023,423 could significantly reduce the thermal hyperalgesia that was induced by i.p. injection of pge(2). cj-023,423 was also effective in models of acute and chronic inflammatory pain. in addition, cj-023,423 was able to significantly reduce mechanical hyperalgesia in the carrageenan model. furthermore, cj-023,423 reversed complete freund's adjuvant-induced chronic inflammatory pain response significantly [1].

References

[1] KAZUNARI NAKAO. CJ-023,423, a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties.[J]. ACS Applied Electronic Materials, 2007: 686-694. DOI:10.1124/jpet.107.122010
[2] TAKAKO OKUMURA. Effects of the selective EP4 antagonist, CJ-023,423 on chronic inflammation and bone destruction in rat adjuvant-induced arthritis[J]. Journal of Pharmacy and Pharmacology, 2010, 60 6: 723-730. DOI:10.1211/jpp.60.6.0007
[3] Q CHEN. A novel antagonist of the prostaglandin E(2) EP(4) receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models.[J]. British Journal of Pharmacology, 2010, 160 2: 292-310. DOI:10.1111/j.1476-5381.2010.00647.x
[4] DINGZHI WANG R D. The Role of Prostaglandin E(2) in Tumor-Associated Immunosuppression.[J]. Trends in molecular medicine, 2016, 22 1 1: 1-3. DOI:10.1016/j.molmed.2015.11.003
[5] NCT03696212 and NCT03658772

Grapiprant Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Grapiprant manufacturers

Hpets Biotech Company (Chongqing) Co.,ltd

Product: Grapiprant 415903-37-6
Price: US $0.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100 tons
Release date: 2023-03-21

Hangzhou ICH Biofarm Co., Ltd

Product: Grapiprant 415903-37-6
Price: US $0.00-0.00/g
Min. Order: 1g
Purity: 98% HPLC
Supply Ability: 500kh
Release date: 2023-06-29

415903-37-6, GrapiprantRelated Search:

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N-((4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenethyl)carbamoyl)-4-methylbenzenesulfonamide

CJ-023423

Grapiprant

2-Ethyl-4,6-dimethyl-1-[4-[2-[[[[(4-methylphenyl)sulfonyl]amino]carbonyl]amino]ethyl]phenyl]-1H-imidazo[4,5-c]pyridine

AAT 007

MR 10A7

RQ 00000007

RQ 7

Grapiprant (CJ-023423)

1-[2-[4-(2-ethyl-4,6-dimethylimidazo[4,5-c]pyridin-1-yl)phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea

CAS#415903-37-6

CJ-023423; CJ 023423; CJ023423; CAS#415903-37-6; RQ-00000007; RQ 00000007; RQ00000007; AAT-007; AAT007; AAT 007; GRAPIPRANT

CS-1556

GRAPIPRANT;RQ-00000007;AAT-007

Grprant

N-[[2,4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenylethylamino]carbonyl]-4-methyl-benzenesulfonamide

RQ 00000007,Inhibitor,Grapiprant,CJ 023423,RQ00000007,Prostaglandin Receptor,AAT 007,inhibit,AAT007,CJ023423

Grapiprant, CJ-023423, AAT-007

Grapiprant, 10 mM in DMSO

Grapiron

Graprant

Koplante

415903-37-6

API