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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;CJ-023423;Grapiprant;RQ 00000007;CAS#415903-37-6
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)

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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, EP1-4. EP4 is a Gs 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 (Ki = 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) Nakao?et al.?(2007),?CJ-023,423, a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties;?J. Pharmacol. Exp. Ther.?332?686 2) Okumura?et al.?(2008),?Effects of the selective EP4 antagonist, CJ-023,423 on chronic inflammation and bone destruction in rat adjuvant-induced arthritis;?J. Pharm. Pharmacol.?60?7235 3) Chen?et al.?(2010),?A novel antagonist of the prostaglandin E2 EP4 receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models;?Br. J. Pharmacol.?160?292 4) Wang and DuBois (2016),?Wang and DuBois (2016), The Role of Prostaglandin E2 in Tumor-Associated Immunosuppression;?Trends Mol. Med.?22?1 5) NCT03696212 and NCT03658772

Grapiprant Preparation Products And Raw materials

Raw materials

Preparation Products

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Grapiprant Suppliers

China 93 China Hong Kong 1 India 2 United States 11 Global 107
MedChemexpress LLC
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021-58955995
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609-228-5909
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sales@medchemexpress.cn
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United States
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Musechem
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+1-800-259-7612
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+1-800-259-7612
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info@musechem.com
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United States
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InvivoChem
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+1-708-310-1919 +1-13798911105
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708-557-7486
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sales@invivochem.cn
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United States
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Cckinase, Inc.
Tel
+1 (732)236-3202
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sales@cckinase.com
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United States
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2738
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BOC Sciences
Tel
+1-631-485-4226
Fax
1-631-614-7828
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inquiry@bocsci.com
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United States
ProdList
19553
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Aladdin Scientific
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+1-+1(833)-552-7181
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sales@aladdinsci.com
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United States
ProdList
57505
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58
ApexBio Technology
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BOC Sciences
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United States
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Focus Biomolecules
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Cayman Chemical Company
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cayman@caymanchem.com
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United States
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United States Biological
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chemicals@usbio.net
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United States
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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
  • 415903-37-6
  • API