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  1. Membrane Transporter/Ion Channel Neuronal Signaling Protein Tyrosine Kinase/RTK GPCR/G Protein
  2. TRP Channel Insulin Receptor CGRP Receptor
  3. BCTC

BCTC 是口服有效的香草素受體1型 (VR1) 電流抑制劑。BCTC 是瞬時(shí)受體電位陽(yáng)離子通道亞家族 M 成員 8 (TRPM8 ) 和瞬時(shí)受體電位香草素1 (TRPV1 ) 拮抗劑。BCTC 是胰島素增敏劑和分泌劑。BCTC 具有抗癌、鎮(zhèn)痛作用。

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BCTC Chemical Structure

BCTC Chemical Structure

CAS No. : 393514-24-4

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10 mM * 1 mL in DMSO ¥660
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5 mg ¥600
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10 mg ¥800
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50 mg ¥2800
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查看 TRP Channel 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

BCTC is an orally active current inhibitor of vanilloid receptor type 1 (VR1). BCTC is a transient receptor potential cation channel subfamily M member 8 (TRPM8) and transient receptor potential vanilloid 1 (TRPV1) antagonist. BCTC is an insulin sensitizer and secretor. BCTC has anticancer and analgesic effects[1][2][3][4][5].

IC50 & Target

IC50: 37.0 nM (CGRP-LI)[3].
IC50: 36.0 nM (SP-LI)[3].

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
0.5 nM
Compound: 5
Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay
Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay
[PMID: 17489570]
CHO IC50
0.6 nM
Compound: 5
Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay
Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay
[PMID: 17489570]
CHO IC50
0.7 nM
Compound: 5
Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay
Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay
[PMID: 17489570]
CHO IC50
0.7 nM
Compound: 5
Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay
Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay
[PMID: 17489570]
CHO-K1 IC50
0.019 μM
Compound: BCTC
Antagonist activity at capsaicin-induced human recombinant TRPV1 expressed in CHO-K1 cells co-expressing aequorin incubated for 2.5 mins in presence of ATP followed by capsaicin addition by luminescence assay
Antagonist activity at capsaicin-induced human recombinant TRPV1 expressed in CHO-K1 cells co-expressing aequorin incubated for 2.5 mins in presence of ATP followed by capsaicin addition by luminescence assay
[PMID: 31202991]
HEK293 IC50
0.6 nM
Compound: 5
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay
[PMID: 17489570]
HEK293 IC50
0.6 nM
Compound: 5
Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay
Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay
[PMID: 17489570]
HEK293 IC50
1.9 nM
Compound: 5
Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
[PMID: 17489570]
HEK293 IC50
475 nM
Compound: BCTC
Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of menthol mediated current amplitude at +80 mV holding potential by whole cell patch-clamp assay
Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of menthol mediated current amplitude at +80 mV holding potential by whole cell patch-clamp assay
[PMID: 26847872]
HEK293 IC50
5 nM
Compound: 5
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
[PMID: 17489570]
HEK-293T IC50
0.15 nM
Compound: BCTC
Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-based assay
Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-based assay
[PMID: 24484240]
HEK-293T IC50
2.12 nM
Compound: BCTC
Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of temperature-induced calcium flux after 30 mins by Fluo-4AM based fluorescence assay
Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of temperature-induced calcium flux after 30 mins by Fluo-4AM based fluorescence assay
[PMID: 23796768]
HEK-293T IC50
4.86 nM
Compound: BCTC
Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of capsaicin-induced calcium flux after 30 mins by Fluo-4AM based fluorescence assay
Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of capsaicin-induced calcium flux after 30 mins by Fluo-4AM based fluorescence assay
[PMID: 23796768]
體外研究
(In Vitro)

BCTC (20-100 μM; 72 h) 對(duì) DU145 細(xì)胞有高選擇性的抗腫瘤活性[1]
BCTC (20-100 μM; 48 h) 通過選擇性的調(diào)節(jié)細(xì)胞周期調(diào)節(jié)蛋白亞群的表達(dá)水平來誘導(dǎo)細(xì)胞周期阻滯在G0/G1 期,且不引發(fā)細(xì)胞凋亡[1]。
BCTC (10 μM 和 100 μM; 48 h) 抑制細(xì)胞的遷移和侵襲[1]
BCTC (3-300 nM) 可以通過抑制辣椒素 (300 nM) 誘導(dǎo)的大鼠脊髓切片中降鈣素基因相關(guān)肽樣免疫反應(yīng)性 (CGRP-LI) (IC50=37.0 nM) 和 p 樣物質(zhì)免疫反應(yīng)性 (SP-LI) (IC50=36.0 nM) 的釋放,從而有效抑制大鼠脊髓 TRPV1 功能[3]

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

Western Blot Analysis[1]

Cell Line: DU145
Concentration: 20 μM, 40 μM, 60 μM, 80 μM,100 μM
Incubation Time: 48 h
Result: Down-regulated p-Akt, while p-GSK-3β was up-regulated leaving their unphosphorylated form unchanged.
Significantly down-regulated Cyclin D1(20), the most relevant protein in the cell cycle, without affecting cyclin-B1.
Reduced the expression of CDK2 and CDK6, but without affecting the expression level of CDK4.
Downregulates MMP2 and p-FAK levels.

Cell Viability Assay[1]

Cell Line: DU145, PNT1A
Concentration: 20 μM, 40 μM, 60 μM, 80 μM,100 μM
Incubation Time: 72 h
Result: Decreased the growth of DU145 cells in a concentration-dependent manner, with 12.03% and 50.69% growth inhibition at 10 μM and 100 μM, respectively, but had little effect on normal prostate PNT1A cells.
體內(nèi)研究
(In Vivo)

BCTC (1-30 mg/kg; 口服給藥; 單劑量) 可以通過靶向 VR1 來抑制 Sprague-Dawley 大鼠的炎癥性和神經(jīng)性的熱痛覺和機(jī)械性痛覺過敏,具有鎮(zhèn)痛作用[2]。
BCTC (10-100 mg/kg; 口服給藥,一天2次連續(xù)4周) 可以改善糖尿病 ob/ob 小鼠的胰島素抵抗和全身糖脂代謝,增加胰島素的分泌[5]。

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

Animal Model: Capsaicin-induced Sprague-Dawley rats model[2]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral gavage (p.o.), Single dose. Before capsaicin (HY-10448) treatment (30 μg; intraplantar injection; Single dose)
Result: Inhibited capsaicin-mediated thermal hyperalgesia in a dose-dependent manner.
Animal Model: Freund’s complete adjuvant (FCA) Sprague-Dawley rats model[2]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral gavage (p.o.), Single dose. After 100 % FAC treatment (50 μL; intraplantar injection; Single dose)
Result: Significantly reduced FAC-induced inflammation-related thermal pain and mechanical hyperalgesia, and extended the inhibitory effect of mechanical hyperalgesia to 6 h at high doses (10 mg/kg, 30 mg/kg).
Animal Model: Partial sciatic nerve ligation Sprague-Dawley rats model[2]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral gavage (p.o.), Single dose. After partial sciatic nerve ligation.
Result: Reduced post-operative abnormal tactile pain and mechanical hyperalgesia in a dose-dependent manner.
Animal Model: Particularly strong insulin resistance and hyperinsulinemia ob/ob mice model[5]
Dosage: 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration: Oral gavage (p.o.); Twice daily for 4 weeks
Result: Reduced plasma triglyceride and glucose area under the curve (AUC) level.
Decreased calcitonin gene-related peptide (CGRP) levels in a dose-dependent manner.
分子量

372.89

Formula

C20H25ClN4O

CAS 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : ≥ 50 mg/mL (134.09 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.6818 mL 13.4088 mL 26.8176 mL
5 mM 0.5364 mL 2.6818 mL 5.3635 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.70 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.70 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中,混合均勻。

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 98.03%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6818 mL 13.4088 mL 26.8176 mL 67.0439 mL
5 mM 0.5364 mL 2.6818 mL 5.3635 mL 13.4088 mL
10 mM 0.2682 mL 1.3409 mL 2.6818 mL 6.7044 mL
15 mM 0.1788 mL 0.8939 mL 1.7878 mL 4.4696 mL
20 mM 0.1341 mL 0.6704 mL 1.3409 mL 3.3522 mL
25 mM 0.1073 mL 0.5364 mL 1.0727 mL 2.6818 mL
30 mM 0.0894 mL 0.4470 mL 0.8939 mL 2.2348 mL
40 mM 0.0670 mL 0.3352 mL 0.6704 mL 1.6761 mL
50 mM 0.0536 mL 0.2682 mL 0.5364 mL 1.3409 mL
60 mM 0.0447 mL 0.2235 mL 0.4470 mL 1.1174 mL
80 mM 0.0335 mL 0.1676 mL 0.3352 mL 0.8380 mL
100 mM 0.0268 mL 0.1341 mL 0.2682 mL 0.6704 mL
Help & FAQs
  • 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.

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Inquiry Information

產(chǎn)品名稱:
BCTC
目錄號(hào):
HY-19960
需求量: