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
- Molecular Weight:
- 491.61
- MOL File:
- 415903-37-6.mol
- Modify Date:
- 2024/3/5 13:23:38
| 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. |
| 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 |
Grapiprant Chemical Properties,Uses,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).
Grapiprant Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Zenfold Sustainable Technologies (ZST) | +91-9945888778 +91-9945888778 | Karnataka, India | 32 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| Hpets Biotech Company (Chongqing) Co.,ltd | +8613340353813 | China | 26 | 58 | Inquiry |
| Hangzhou ICH Biofarm Co., Ltd | +86-0571-28186870; +undefined8613073685410 | China | 985 | 58 | Inquiry |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32760 | 60 | Inquiry |
| BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
| ANHUI WITOP BIOTECH CO., LTD | +8615255079626 | China | 23556 | 58 | Inquiry |
| Guangzhou TongYi biochemistry technology Co.,LTD | +8613073028829 | China | 2996 | 58 | Inquiry |
| InvivoChem | +1-708-310-1919 +1-13798911105 | United States | 6393 | 58 | Inquiry |
| Nanjing Doge Biomedical Technology Co., Ltd | +86-25-58227606 +86-15305155328 | China | 4128 | 58 | Inquiry |
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