SML2411

KPR-2579

≥98% (HPLC)

• 別名: (αR)-α-[Benzoyl[(1R)-1-(3,5-difluorophenyl)ethyl]amino]-benzeneacetamide, N-((R)-2-Amino-2-oxo-1-phenylethyl)-N-((R)-1-(3,5-difluorophenyl)ethyl)benzamide, N-((R)-Carbamoylphenylmethyl)-N-[(R)-1-(3,5-difluorophenyl)ethyl]benzamide
• 実験式（ヒル表記法）: C₂₃H₂₀F₂N₂O₂
• CAS番号: 1801742-41-5
• 分子量: 394.41
• UNSPSCコード: 12352200

特性

• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 光学活性: [α]/D +124 to +136°, c = c=1 in chloroform-d
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear
• 保管温度: 2-8°C
• SMILES記法: O=C(C1=CC=CC=C1)N([C@H](C)C2=CC(F)=CC(F)=C2)[C@H](C3=CC=CC=C3)C(N)=O
• InChI: 1S/C23H20F2N2O2/c1-15(18-12-19(24)14-20(25)13-18)27(23(29)17-10-6-3-7-11-17)21(22(26)28)16-8-4-2-5-9-16/h2-15,21H,1H3,(H2,26,28)/t15-,21-/m1/s1
• InChI Key: NNXPFEMWLZLAHM-QVKFZJNVSA-N

詳細

生物化学的／生理学的作用

KPR-2579 does not distress temperature of the body at any given dose. It helps to block the activation of C-fiber single-unit afferent activities (SAAs), stimulated by acetic acid (AA).

KPR-2579 is a potent and selective transient receptor potential melastatin 8 (TRPM8; CRM1) antagonist (IC50 = 80/89 nM against EC80 MeOH-induced Ca²⁺ response in human/rat CRM1 HEK293T transfectants) with good selectivity (IC50 >30 μM against ligand-induced Ca²⁺ influx using hTRPA1, hTRPV1, or hTRPV4 transfectants) and oral availability (59% post 10 mg/kg p.o.; rats). KPR-2579 exhibits in vivo efficacy against icilin-induced wet-dog shakes (WDS; by 31/73/100% with 1/3/10 mg/kg p.o. 1h prior to icilin i.p.; female rats) and distension-induced rhythmic bladder contraction (by 70/89% with 0.1/0.3 mg/kg i.v.; male rats) without negative cardiovascular effects.

Potent and selective transient receptor potential melastatin 8 (TRPM8; CRM1) antagonist with good selectivity, in vivo efficacy and oral bioavailability.

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable