2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. KJM429

KJM429 (MK-056) 是一种高亲和力的大鼠香草酸受体 rTRPV1 的配体 (Ki=30-62.6 nM)，具有独特的双重调节功能。KJM429 既能竞争性拮抗由 Capsaicin (HY-10448)、Resiniferatoxin (HY-N2333)、热刺激及弱酸 (pH 6.0) 诱导的 TRPV1 受体激活，又在强酸环境 (pH<5.5) 下转变为 TRPV1 激动剂。KJM429 能有效阻断 Capsaicin 及部分热刺激诱导的钙内流，并在低 pH 条件下诱发钙摄取，对非 TRPV1 介导的钙信号影响极小。KJM429 可用于带状疱疹后神经痛、糖尿病神经病变、丛集性头痛、骨关节炎及瘙痒症等疼痛相关疾病机制的研究。

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KJM429

KJM429 Chemical Structure

CAS No. : 401907-57-1

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KJM429 相关抗体

Top Publications Citing Use of Products

查看 TRP Channel 亚型特异性产品:

查看所有亚型
TRPA1 TRPC3 TRPC4 TRPC5 TRPM8 TRPM2 TRPM3 TRPM4 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KJM429 (MK-056) is a high-affinity ligand for the rat vanilloid receptor rTRPV1 (Ki=30-63 nM) with a unique dual regulatory function. KJM429 acts as a competitive antagonist to inhibit TRPV1 receptor activation induced by Capsaicin (HY-10448), resiniferatoxin, thermal stimulation and weak acid (pH 6.0), and switches to a TRPV1 agonist under strong acid conditions (pH<5.5). KJM429 effectively blocks calcium influx induced by Capsaicin and partial thermal stimulation, and triggers calcium uptake under low pH conditions, with minimal effects on non-TRPV1-mediated calcium signaling. KJM429 can be used for research on the mechanisms of pain-related diseases such as postherpetic neuralgia, diabetic neuropathy, cluster headache, osteoarthritis and pruritus[1].

IC50 & Target

rTRPV1

 

体外研究
(In Vitro)

KJM429 抑制表达 rTRPV1 的中国仓鼠卵巢细胞中 Capsaicin (HY-10448)、Resiniferatoxin (HY-N2333) 诱导的钙摄取，其 Ki 分别为 53.9 nM 和 30.4 nM[1]。
KJM429 (50-400 nM; 5 min) 可作为中国仓鼠卵巢细胞中 rTRPV1 的竞争性拮抗剂，对 Capsaicin 的 Ki 值为 31.2 nM，对 Resiniferatoxin 的 Ki 值为 35.2 nM[1]。
KJM429 (0.3-3000 nM; 5 min) 可部分抑制表达 rTRPV1 的中国仓鼠卵巢细胞中热诱导的钙摄取，在 3000 nM 时可使摄取量降低 65.4%[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

KJM429 相关抗体:
分子量

405.58

Formula

C20H27N3O2S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

KJM429 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KJM429401907-57-1MK-056KJM 429KJM-429MK056MK 056TRP ChannelTransient receptor potential channelsrat vanilloid receptor 1rat dorsal root ganglion neuronsosteoarthritisrVR1resiniferatoxindiabetic neuropathycultured neuronspostherpetic neuralgiaChinese hamster ovary cellscapsaicinInhibitorinhibitorinhibit

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HY-165459
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