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  2. Membrane Transporter/Ion Channel
  3. Na+/Ca2+ Exchanger
  4. YM-244769 hydrochloride

YM-244769 hydrochloride 是一種有效的、選擇性的、具有口服活性的 Na+/Ca2+ 交換體 (NCX) 抑制劑。YM-244769 hydrochloride 優(yōu)先抑制 NCX3，抑制 NCX 單向向外電流 (Ca2+ 進入模式)，IC50 分別為 18 nM 和 50 nM。YM-244769 hydrochloride 可有效預(yù)防缺氧/復(fù)氧誘導(dǎo)的 SH-SY5Y 神經(jīng)元細胞損傷。YM-244769 hydrochloride 還能增加小鼠的尿量和尿液中電解質(zhì)的排泄。

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YM-244769 hydrochloride Chemical Structure

YM-244769 hydrochloride Chemical Structure

CAS No. : 837424-39-2

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5 mg ￥1600
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10 mg ￥2600
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25 mg ￥4900
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Customer Review

Other Forms of YM-244769 hydrochloride:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

YM-244769 hydrochloride is a potent, selective and orally active Na+/Ca2+ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice[1][2][3].

IC50 & Target

IC50: 18 nM (NCX3)[1]
體外研究
(In Vitro)

YM-244769 (0.003-1 μM) 劑量依賴性地抑制 NCX1、NCX2 和 NCX3 轉(zhuǎn)染細胞對 45Ca2+ 的初始攝取速率，其 IC50 值分別為 68 、96 和 18 nM[1]。
YM-244769 (0.3 或 1 μM) 可有效保護 SH-SY5Y 細胞和 LLC-PK1 細胞免受缺氧/復(fù)氧誘導(dǎo)的乳酸脫氫酶 (LDH) 釋放 (1 μM)[1]。
YM-244769 具有反向模式選擇性[1]。
YM-244769 (1 和 10 μM) 以濃度和細胞內(nèi) [Na+]i 依賴方式抑制 NCX 電流 (INCX)。針對單向外向 NCX 電流 (即鈣離子內(nèi)流模式) 的 IC50 為 0.05 μM。針對雙向向外和向內(nèi) INCX 的 IC50 值相似，約為 100 nM，Hill 系數(shù)約為 1[3]。
YM-244769 對胰蛋白酶不敏感[3]。

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

YM-244769 (0.1-1 mg/kg；口服 ；單劑量) 在小鼠中表現(xiàn)出劑量依賴性的利鈉作用，并顯著增加尿中 Ca2+ 的排泄量以及 Ca2+/肌酐 (Cr) 的比值[2]。

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

Animal Model: Wild-type C57BL/6J mice and NCX-KO mice[2]
Dosage: 0.1, 0.3 and 1 mg/kg
Administration: Oral administration, once
Result: Caused a dose-dependent increase (up to approximately 200%) in urine volume and urinary excretion of electrolytes (Na+, K+ and Cl-). Natriuretic actions were equivalently observed in NCX1-KO and WT, but disappeared in NCX2-KO and double KO.
分子量

479.93

Formula

C26H23ClFN3O3
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
純度 & 產(chǎn)品資料
參考文獻

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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：
YM-244769 hydrochloride
目錄號：
HY-107659
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