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  2. Metabolic Enzyme/Protease Autophagy
  3. Dipeptidyl Peptidase Autophagy
  4. Sitagliptin phosphate

Sitagliptin phosphate  (Synonyms: 磷酸西他列汀; MK-0431 phosphate)

目錄號(hào): HY-13749A 純度: 99.64%
COA 產(chǎn)品使用指南 技術(shù)支持

Sitagliptin phosphate (MK-0431 phosphate) 是一種有效的 DPP4 抑制劑，在 Caco-2 細(xì)胞中，IC50 值為 19 nM。

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Sitagliptin phosphate Chemical Structure

Sitagliptin phosphate Chemical Structure

CAS No. : 654671-78-0

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥476
In-stock
25 mg ￥433
In-stock
50 mg ￥623
In-stock
100 mg ￥880
In-stock
200 mg ￥1280
In-stock
500 mg ￥2088
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1 g   詢價(jià)  
5 g   詢價(jià)  

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Other Forms of Sitagliptin phosphate:

查看 Dipeptidyl Peptidase 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[1].

IC50 & Target

DPP-4

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
11 μM
Compound: MK-0431
Inhibition of human DPP8 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
Inhibition of human DPP8 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
[PMID: 22853995]
HEK293 IC50
20 μM
Compound: MK-0431
Inhibition of human DPP9 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
Inhibition of human DPP9 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
[PMID: 22853995]
HEK293 IC50
22 nM
Compound: Sitagliptin Phosphate
Inhibition of recombinant human DPP-4 expressed in HEK293 cells using H-Gly-Pro-AMC as substrate measured over 15 mins by fluorescence analysis
Inhibition of recombinant human DPP-4 expressed in HEK293 cells using H-Gly-Pro-AMC as substrate measured over 15 mins by fluorescence analysis
[PMID: 28128944]
HEK293 IC50
6 nM
Compound: MK-0431
Inhibition of human DPP4 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
Inhibition of human DPP4 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins
[PMID: 22853995]
體外研究
(In Vitro)

Sitagliptin phosphate 對(duì) Caco-2 細(xì)胞提取物中的 DPP-4 表現(xiàn)出有效的抑制作用，IC50 為 19 nM[1]。西格列汀通過(guò)涉及 cAMP/PKA/Rac1 激活的通路減少分離的脾臟 CD4 T 細(xì)胞的體外遷移[2]。最近的一項(xiàng)研究表明，西格列汀發(fā)揮一種新穎的直接作用，通過(guò) DPP-4 獨(dú)立的、蛋白激酶 A 和 MEK-ERK1/2 依賴的途徑刺激腸道 L 細(xì)胞分泌 GLP-1。因此，它降低了自身免疫對(duì)移植物存活的影響[3]。

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

在自由喂養(yǎng)的 Han-Wistar 體內(nèi)，Sitagliptin phosphate 抑制血漿 DPP-4 活性的 ED50 值計(jì)算為給藥后 7 小時(shí) 2.3 mg/kg 和給藥后 24 小時(shí) 30 mg/kg大鼠[1]。
鏈脲佐菌素誘導(dǎo)的 1 型糖尿病小鼠模型顯示血漿中 DPP-4 水平升高，這在服用 Sitagliptin phosphate 飲食的小鼠中可被顯著抑制。這是通過(guò)對(duì)高血糖癥的調(diào)節(jié)產(chǎn)生積極影響來(lái)實(shí)現(xiàn)的，可能是通過(guò)延長(zhǎng)胰島移植物的存活[4]。
Sitagliptin phosphate 的血漿清除率和分布容積在大鼠中 (40-48 mL/min/kg，7-9 L/kg) 高于狗 (9 mL/min/kg，3 L/kg)；其半衰期在大鼠中較短，為 2 小時(shí)，而在狗中為 4 小時(shí)[5]。

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

505.31

Formula

C16H18F6N5O5P
CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

磷酸西他列汀
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

4°C, sealed storage, away from moisture and light

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (197.90 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(kāi)封的 DMSO)

H2O 中的溶解度 : 50 mg/mL (98.95 mM; 超聲助溶)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量