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  2. GPCR/G Protein
  3. LPL Receptor
  4. NIBR0213

NIBR-0213 是一種有效的、具有口服活性的選擇性 S1P1 拮抗劑，對實驗性自身免疫性腦脊髓炎有效。在 GTPγ35S 試驗中，NIBR-0213 有效作用于人和大鼠 S1P1，IC50 分別為 2.0 nM 和 2.3 nM。

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NIBR0213 Chemical Structure

NIBR0213 Chemical Structure

CAS No. : 1233332-14-3

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規(guī)格 價格 是否有貨 數(shù)量
5 mg ￥1350
In-stock
10 mg ￥2100
In-stock
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100 mg   詢價  

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Customer Review

查看 LPL Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

NIBR-0213 is a potent, orally active and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively) in GTPγ35S assays[1].

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
> 10 μM
Compound: 38, NIBR-0213
Antagonist activity at human S1P5 receptor expressed in CHO cells after 120 mins by [35S]GTPgammaS binding assay
Antagonist activity at human S1P5 receptor expressed in CHO cells after 120 mins by [35S]GTPgammaS binding assay
[PMID: 24125884]
CHO IC50
> 10 μM
Compound: 38, NIBR-0213
Antagonist activity at human S1P4 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 20 mins by Fluo-4/FLIPR method
Antagonist activity at human S1P4 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 20 mins by Fluo-4/FLIPR method
[PMID: 24125884]
CHO IC50
> 10 μM
Compound: 38, NIBR-0213
Antagonist activity at human S1P3 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 20 mins by Fluo-4/FLIPR method
Antagonist activity at human S1P3 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 20 mins by Fluo-4/FLIPR method
[PMID: 24125884]
CHO IC50
> 10 μM
Compound: 38, NIBR-0213
Antagonist activity at human S1P2 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 20 mins by Fluo-4/FLIPR method
Antagonist activity at human S1P2 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 20 mins by Fluo-4/FLIPR method
[PMID: 24125884]
CHO IC50
2 nM
Compound: 38, NIBR-0213
Antagonist activity at human S1P1 receptor expressed in CHO cells after 120 mins by [35S]GTPgammaS binding assay
Antagonist activity at human S1P1 receptor expressed in CHO cells after 120 mins by [35S]GTPgammaS binding assay
[PMID: 24125884]
體外研究
(In Vitro)

NIBR-0213 對 hS1P1 表現(xiàn)出抑制活性，IC50 為 2.5 nM，而在 Ca2+ 動員試驗中對 S1P2、S1P3 和 S1P4 無活性（IC50 >10 μM）[1]。
NIBR-0213 在 GTPγ35S 試驗中對人類和大鼠 S1P1（IC50 分別為 2.0 nM 和 2.3 nM）表現(xiàn)出強效且相當?shù)男Я?，而對小?S1P1 的 IC50 為 8.5 nM[1]。
NIBR-0213 對人類 S1P5 顯示出約 3,000 倍的選擇性 GTPγ35S 測定[1]。
NIBR-0213 是一種競爭性 S1P1 拮抗劑，計算出的 Kd 為 0.37±0.031 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

NIBR-0213（大鼠口服 30 mg/kg）可在 14 小時內(nèi)使外周血淋巴細胞 (PBL) 計數(shù)降低 75%-85%，且這種效果可持續(xù)至治療后 24 小時[1]。
NIBR-0213（30 mg/kg 和 60 mg/kg）在小鼠實驗性自身免疫性腦脊髓炎 (EAE) 模型中治療有效[1]。
NIBR-0213 的 PK 特性顯示其具有中等清除率（26 mL/min/kg）和高口服生物利用度（69%），口服給藥后可產(chǎn)生顯著的暴露量[1]。

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

Animal Model: Lewis or Wistar rats (220-250 g, males)[1]
Dosage: 30?mg/kg
Administration: Orally
Result: Reduced the PBL counts by 75%-85% within 14?hr and maintained this effect up to 24?hr posttreatment.
Animal Model: C57BL/6 mice bearing EAE model[1]
Dosage: 30?mg/kg and 60?mg/kg
Administration: 30?mg/kg twice per day (BID) for 3?days and then increased to 60?mg/kg BID until the remainder of the experiment. In total, the treatment lasted 26?days
Result: Resulted in a gradual reduction in disease-scores, with a divergence from vehicle controls that became significant after 5?days.
分子量

464.98

Formula

C27H29ClN2O3
CAS 號
性狀

固體

顏色

Off-white to light yellow

運輸條件

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

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 125 mg/mL (268.83 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

Ethanol 中的溶解度 : ≥ 25 mg/mL (53.77 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.1506 mL 10.7532 mL 21.5063 mL
5 mM 0.4301 mL 2.1506 mL 4.3013 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.38%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.1506 mL 10.7532 mL 21.5063 mL 53.7658 mL
5 mM 0.4301 mL 2.1506 mL 4.3013 mL 10.7532 mL
10 mM 0.2151 mL 1.0753 mL 2.1506 mL 5.3766 mL
15 mM 0.1434 mL 0.7169 mL 1.4338 mL 3.5844 mL
20 mM 0.1075 mL 0.5377 mL 1.0753 mL 2.6883 mL
25 mM 0.0860 mL 0.4301 mL 0.8603 mL 2.1506 mL
30 mM 0.0717 mL 0.3584 mL 0.7169 mL 1.7922 mL
40 mM 0.0538 mL 0.2688 mL 0.5377 mL 1.3441 mL
50 mM 0.0430 mL 0.2151 mL 0.4301 mL 1.0753 mL
DMSO 60 mM 0.0358 mL 0.1792 mL 0.3584 mL 0.8961 mL
80 mM 0.0269 mL 0.1344 mL 0.2688 mL 0.6721 mL
100 mM 0.0215 mL 0.1075 mL 0.2151 mL 0.5377 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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產(chǎn)品名稱：
NIBR0213
目錄號：
HY-18166
需求量：