SML2411
KPR-2579
≥98% (HPLC)
别名:
(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
登录 查看组织和合同定价。
选择规格
变更视图
关于此项目
Assay:
≥98% (HPLC)
Form:
powder
assay
≥98% (HPLC)
form
powder
optical activity
[α]/D +124 to +136°, c = c=1 in chloroform-d
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
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
Biochem/physiol Actions
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable