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  1. GPCR/G Protein Neuronal Signaling
  2. Neurotensin Receptor
  3. NTRC-824

NTRC-824 (Compound 5) 是一種有效的,選擇性的,類似于神經(jīng)降壓素的非肽神經(jīng)降壓素受體 2 型 (NTS2) 拮抗劑,IC50 為 38 nM,Ki 為 202 nM。NTRC-824 對(duì) NTS2 的選擇性是 NTS1 (Ki >30 μM) 的 150 倍以上。

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NTRC-824 Chemical Structure

NTRC-824 Chemical Structure

CAS No. : 1623002-61-8

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查看 Neurotensin Receptor 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

NTRC-824 (Compound 5) is a potent, selective and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist with an IC50 of 38 nM and a Ki of 202 nM. NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (Ki >30 μM)[1].

IC50 & Target

IC50: 38 nM (Nurotensin receptor type 2)[1]
Ki: 202 nM (Nurotensin receptor type 2)[1]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO-K1 IC50
38 nM
Compound: 5
Antagonist activity at rat NTS2 receptor expressed in CHO-K1 cells assessed as inhibition of SR142948a-induced calcium mobilization by FLIPR assay
Antagonist activity at rat NTS2 receptor expressed in CHO-K1 cells assessed as inhibition of SR142948a-induced calcium mobilization by FLIPR assay
[PMID: 25157640]
體外研究
(In Vitro)

Testing of NTRC-824 (Compound 5) at the NTS1 receptor shows no binding activity in the NTS1 assay up to 30 μM, making NTRC-824 (Compound 5) selective for NTS2 in both the binding and functional assays. NTRC-824 (Compound 5) is the first nonpeptide compound that behaves like, and is more active than, the endogenous ligand[1].

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

分子量

553.55

Formula

C25H26F3N3O6S

CAS 號(hào)
性狀

固體

顏色

Off-white to light yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 1 mg/mL (1.81 mM; 超聲加熱助溶; 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 1.8065 mL 9.0326 mL 18.0652 mL
5 mM --- --- ---
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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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 1.8065 mL 9.0326 mL 18.0652 mL 45.1630 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:
NTRC-824
目錄號(hào):
HY-12436
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