THIQ

目錄號(hào): HY-10624 純度: 98.28%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

THIQ 是 MC4R 的第一選擇激動(dòng)劑，對(duì) hMC4R (IC₅₀=1.2 nM; EC₅₀=2.1 nM) 和 rMC4R(IC₅₀=0.6 nM; EC₅₀=2.9 nM) 具有較高的親和力和效價(jià)。THIQ 對(duì) MC1R、MC3R 和 MC5R 有較低效價(jià)，在引起嚙齒動(dòng)物勃起活動(dòng)中起作用。THIQ 作為 MC4R 的一種活性分子過(guò)氧化物酶體，挽救了一些細(xì)胞內(nèi)保留的 MC4R 突變體的細(xì)胞表面表達(dá)和信號(hào)傳導(dǎo)。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

THIQ Chemical Structure

CAS No. : 312637-48-2

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1 mg	￥491	In-stock
5 mg	￥1000	In-stock
10 mg	￥1600	In-stock
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50 mg	￥4800	In-stock
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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

•Pathol Res Pract. 27 November 2021, 153717.

THIQ 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 Melanocortin Receptor 亞型特異性產(chǎn)品:

查看所有亞型

MC1R MC3R MC2R MC4R MC5R

生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC₅₀=1.2 nM, EC₅₀=2.1 nM) and rMC4R (IC₅₀=0.6 nM, EC₅₀=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants^[1]^[2].

IC₅₀ & Target

MC4R

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BTI-TN-5B1-4	IC₅₀	9 nM Compound: 1	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	[PMID: 14643322]
CHO	IC₅₀	0.6 nM Compound: 1	Evaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells Evaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	[PMID: 12361385]
CHO	IC₅₀	1.2 nM Compound: 1	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	[PMID: 15951175]
CHO	IC₅₀	1.2 nM Compound: 1	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	[PMID: 12361385]
CHO	IC₅₀	1.2 nM Compound: 1	Evaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells Evaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	[PMID: 12361385]
CHO	IC₅₀	1575 nM Compound: 1	Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells Evaluated for binding affinity against rat Melanocortin-5 receptor (rMC5R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	[PMID: 12361385]
CHO	IC₅₀	1883 nM Compound: 1	Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells Evaluated for binding affinity against rat Melanocortin-3 receptor (rMC3R) by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	[PMID: 12361385]
CHO	IC₅₀	2063 nM Compound: 1	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC1R expressed in CHO cells Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC1R expressed in CHO cells	[PMID: 15951175]
CHO	IC₅₀	2067 nM Compound: 1	Evaluated for binding affinity against human melanocortin 1 (hMC1R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells Evaluated for binding affinity against human melanocortin 1 (hMC1R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	[PMID: 12361385]
CHO	IC₅₀	326 nM Compound: 1	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC5R expressed in CHO cells	[PMID: 15951175]
CHO	IC₅₀	326 nM Compound: 1	Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells Evaluated for binding affinity against human melanocortin 5 (hMC5R) receptor by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	[PMID: 12361385]
CHO	IC₅₀	761 nM Compound: 1	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC3R expressed in CHO cells	[PMID: 15951175]
CHO	IC₅₀	761 nM Compound: 1	Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells Evaluated for binding affinity against human Melanocortin-3 receptor (hMC3R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	[PMID: 12361385]
HEK293	EC₅₀	> 1000 nM Compound: 3	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	EC₅₀	0.61 nM Compound: 3	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	EC₅₀	0.71 nM Compound: 3	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	EC₅₀	0.82 nM Compound: 3	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	EC₅₀	1.2 nM Compound: 3	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	EC₅₀	1.5 nM Compound: 3	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	EC₅₀	12 nM Compound: 3	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	EC₅₀	26 nM Compound: 3	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	EC₅₀	3.6 nM Compound: 1	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	[PMID: 14643322]
HEK293	EC₅₀	41 nM Compound: 3	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	EC₅₀	8.5 nM Compound: 3	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]

體外研究
(In Vitro)

THIQ 對(duì)人 MC1R、MC3R 和 MC5R 保持低效力，IC₅₀ 為 2067、761、326 nM，EC₅₀ 分別為 2850, 2487、737 nM。THIQ 在大鼠 MC3R 和 MC5R 中保持低效力，IC₅₀ 為 1883 和 1575 nM，EC₅₀ 為 1325 和 >3000 nM^[1]。
THIQ (10 μM；24 小時(shí)) 使 WT MC4R 的信號(hào)強(qiáng)度降低約 50%，而在 HEK293 細(xì)胞增加三種突變體 (N62S, C84R, and C271Y) ^[2]。

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

體內(nèi)研究
(In Vivo)

THIQ (0.3-10 mg/kg；iv) 劑量依賴性地增加性成熟雄性 Sprague Dawley 大鼠的勃起 (ED₅₀=0.87 mg/kg)。在 5 mg/kg 時(shí)檢測(cè)到勃起次數(shù)的最大增加 (60%)，但與 1 mg/kg 時(shí)沒(méi)有顯著差異。THIQ (20 mg/kg；口服) 還使勃起反應(yīng)顯著增加，平均增加 31±4%^[1]。
THIQ 處理顯示 t_1/2 在 Sprague-Dawley 大鼠中為 0.6 小時(shí) (1 mg/kg，靜脈注射和 10 mg/kg，口服)^[1]。

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

分子量

589.17

Formula

C₃₃H₄₁ClN₆O₂

CAS 號(hào)

312637-48-2

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 : 100 mg/mL (169.73 mM; 超聲助溶; 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)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.6973 mL	8.4865 mL	16.9730 mL
5 mM	0.3395 mL	1.6973 mL	3.3946 mL
10 mM	0.1697 mL	0.8487 mL	1.6973 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.24 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。
以 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。
方案二

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.53 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。

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

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)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(guò) 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(guò)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(guò)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: 98.28%

選擇批次：

Data Sheet (646 KB) SDS (393 KB)

COA (292 KB) HNMR (270 KB) RP-HPLC (269 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Sebhat IK, et al. Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist. J Med Chem. 2002 Oct 10;45(21):4589-93. [Content Brief]

[2]. Huang H, et al. A small molecule agonist THIQ as a novel pharmacoperone for intracellularly retainedmelanocortin-4 receptor mutants. Int J Biol Sci. 2014 Jul 20;10(8):817-24. [Content Brief]

THIQ 相關(guān)分類

Metabolic Disease

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6973 mL	8.4865 mL	16.9730 mL	42.4326 mL
	5 mM	0.3395 mL	1.6973 mL	3.3946 mL	8.4865 mL
	10 mM	0.1697 mL	0.8487 mL	1.6973 mL	4.2433 mL
	15 mM	0.1132 mL	0.5658 mL	1.1315 mL	2.8288 mL
	20 mM	0.0849 mL	0.4243 mL	0.8487 mL	2.1216 mL
	25 mM	0.0679 mL	0.3395 mL	0.6789 mL	1.6973 mL
	30 mM	0.0566 mL	0.2829 mL	0.5658 mL	1.4144 mL
	40 mM	0.0424 mL	0.2122 mL	0.4243 mL	1.0608 mL
	50 mM	0.0339 mL	0.1697 mL	0.3395 mL	0.8487 mL
	60 mM	0.0283 mL	0.1414 mL	0.2829 mL	0.7072 mL
	80 mM	0.0212 mL	0.1061 mL	0.2122 mL	0.5304 mL
	100 mM	0.0170 mL	0.0849 mL	0.1697 mL	0.4243 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.

Keywords:

THIQ312637-48-2Melanocortin ReceptorMC ReceptormelanocortinselectiveelicitingerectileactivitymutantaffinityInhibitorinhibitorinhibit

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