021-51111890
购物车（）
sales@molnova.cn
JNJ-17203212
CAS No. 821768-06-3
JNJ-17203212 ( JNJ17203212 | JNJ 17203212 )
产品货号. M16055 CAS No. 821768-06-3
一种有效的、选择性的、口服生物可利用的 TRPV1 受体拮抗剂，对 hTRPV1 和 rTRPV1 的 IC50 分别为 65 nM 和 102 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥629 | 有现货 |
|
| 10MG | ￥1102 | 有现货 |
|
| 25MG | ￥2465 | 有现货 |
|
| 50MG | ￥3990 | 有现货 |
|
| 100MG | ￥5373 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥692 | 有现货 |
|
生物学信息
-
产品名称JNJ-17203212
-
注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
-
产品简述一种有效的、选择性的、口服生物可利用的 TRPV1 受体拮抗剂，对 hTRPV1 和 rTRPV1 的 IC50 分别为 65 nM 和 102 nM。
-
产品描述A potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively; exhibits high selectivity against a panel of receptors and transporters, and does not inhibits related TRP channels TRPV2, TRPV4, or TRPA1; inhibits both pH (pIC50=7.23) and capsaicin (pIC50=6.32)-induced channel activation; attenuates capsaicin evoked coughs, prevents core hypothermia evoked by capsaicin in vivo.Pain Preclinical.
-
体外实验JNJ-17203212 (0.5 μM) potently inhibits imperatorin-induced TRPV1 activation (Ca2+ increases) in TRPV1-expressing HEK cells.
-
体内实验JNJ-17203212 (0.3 mg/kg; i.v.) dose-dependently reduces inflammatory soup (IS)-induced the immediate early gene c-fos expression.JNJ-17203212 completely blocks capsaicin-induced CGRP (the neurotransmitter calcitonin gene-related peptide) release in a dose-dependent manner. Animal Model:Male Sprague-Dawley rats (260-300 g)Dosage:0.3 mg/kg Administration:Intravenous injection Result:Had a dose-dependent effect on the elevated c-fos expression that occurred after intracisternal injection of IS.
-
同义词JNJ17203212 | JNJ 17203212
-
通路Membrane Transporter/Ion Channel
-
靶点TRP/TRPV Channel
-
受体TRP/TRPV Channel
-
研究领域Neurological Disease
-
适应症Pain
化学信息
-
CAS Number821768-06-3
-
分子量419.3243
-
分子式C17H15F6N5O
-
纯度>98% (HPLC)
-
溶解度10 mM in DMSO
-
SMILESO=C(N1CCN(C2=NC=CC=C2C(F)(F)F)CC1)NC3=NC=C(C(F)(F)F)C=C3
-
化学全称1-Piperazinecarboxamide, 4-[3-(trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-
运输与储存
-
储存条件(-20℃)
-
运输条件With Ice Pack
-
稳定性≥ 2 years
参考文献
1. Swanson DM, et al. J Med Chem. 2005 Mar 24;48(6):1857-72.
2. Bhattacharya A, et al. J Pharmacol Exp Ther. 2007 Nov;323(2):665-74.
3. Cefalu JS, et al. J Urol. 2009 Aug;182(2):776-85.
产品手册
关联产品
-
HC067047 Hydrochlori...
HC-067047 盐酸盐是一种有效的选择性 TRPV4 拮抗剂。
-
RN-1747
RN-1747 是一种选择性瞬时受体电位阳离子通道亚家族 V 成员 4 激动剂（EC50：hTRPV4 为 0.77 μM，mTRPV4 为 4.0 μM，rTRPV4 为 4.1 μM）。 RN-1747 还拮抗 TRPM8（IC50：4 μM）。
-
TRPA1-IN-2
TRPA1-IN-2 (compound 1) 是一种有效的口服活性 TRPA1 抑制剂，IC50 值为 0.04 μM。TRPA1-IN-2 显示出抗炎活性。
