A-317491
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Cat.No：IA4850 Solarbio
CAS：475205-49-3
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Membrane Transporter & Ion Channel > A-317491
Product Information
| CAS | 475205-49-3 |
| Name | A-317491 |
| Molecular Formula | C33H27NO8 |
| Molecular Weight | 565.57 |
| Solubility | Soluble in DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD28044314 |
| SMILES | C1CC(C2=CC=CC=C2C1)N(CC3=CC(=CC=C3)OC4=CC=CC=C4)C(=O)C5=CC(=C(C=C5C(=O)O)C(=O)O)C(=O)O |
| InChIKey | VQGBOYBIENNKMI-LJAQVGFWSA-N |
| InChI | InChI=1S/C33H27NO8/c35-30(25-17-27(32(38)39)28(33(40)41)18-26(25)31(36)37)34(29-15-7-10-21-9-4-5-14-24(21)29)19-20-8-6-13-23(16-20)42-22-11-2-1-3-12-22/h1-6，8-9，11-14，16-18，29H，7，10，15，19H2，(H，36，37)(H，38，39)(H，40，41)/t29-/m0/s1 |
| PubChem CID | 9829395 |
| Target Point | P2X Receptor |
| Passage | Membrane Transporter&Ion Channel |
| Background | A-317491 is A nonnucleotide P2X3 and P2X2/3 receptor antagonist that inhibits calcium flow mediated by it. |
| Biological Activity | A-317491 是一种新型的 P2X3 和 P2X2/3 受体激活非核苷酸拮抗剂，对 hP2X3、rP2X3、hP2X2/3 和 rP2X2/3 的 Kis 分别为 22、22、9 和 92 nM。对其他 P2 受体和其他神经递质受体、离子通道和酶具有高度选择性（IC50>10 μM）。通过阻断 P2X3 和 P2X2/3 受体介导的钙通量，减轻炎症性疼痛和神经病理性疼痛。[1-2] |
| In Vitro | A-317491 potently blocked recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux(Ki = 22-92 nM)and was highly selective(IC50 >10 microM)over other P2 receptors and other neurotransmitter receptors，ion channels，and enzymes. A-317491 also blocked native P2X3 and P2X2/3 receptors in rat dorsal root ganglion neurons.[1] |
| In Vivo | A-317491 dose-dependently(ED50 = 30 micromolkg s.c.)reduced complete Freund's adjuvant-induced thermal hyperalgesia in the rat.[1] In the rat Freund's complete adjuvant model of inflammatory pain，s.c. administration of A-317491 dose-dependently reversed mechanical hyperalgesia. Maximum percent reversal(72%)was seen 3 h after administration at 10 mg/kg. The brain-to-plasma concentration ratio，determined 1 h after 3，10 and 30 mg/kg s.c. dose，indicated limited penetration of A-317491 into the central nervous system.[2] |
| Data Literature Source | [1]. Jarvis MF，et al. A-317491，a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors，reduces chronic inflammatory and neuropathic pain in the rat. Proc Natl Acad Sci U S A. 2002 Dec 24;99(26):17179-84. [2]. Wu G，et al. A-317491，a selective P2X3/P2X2/3 receptor antagonist，reverses inflammatory mechanical hyperalgesia through action at peripheral receptors in rats. Eur J Pharmacol. 2004 Nov 3;504(1-2):45-53. |
| Unit | Bottle |
| Specification | 5mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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