YM 2447690
Modify Date: 2024-01-12 11:51:09
YM 2447690 structure
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Common Name | YM 2447690 | ||
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| CAS Number | 837424-39-2 | Molecular Weight | 516.39100 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C26H24Cl2FN3O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of YM 2447690YM-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]. |
| Name | N-(3-Aminobenzyl)-6-{4-[(3-fluorobenzyl)oxy]phenoxy}nicotinamide dihydrochloride |
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| Description | 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]. |
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| Related Catalog | |
| Target |
IC50: 18 nM (NCX3)[1] |
| In Vitro | YM-244769 (0.003-1 μM) inhibits dose dependently the initial rates of 45Ca2+ uptake into NCX1, NCX2, and NCX3 transfectants with IC50 values of 68 ± 2.9, 96 ± 3.5, and 18 ± 1.0 nM, respectively[1]. YM-244769 (0.3 or 1 μM) efficiently protects against the hypoxia/reoxygenation-induced lactate dehydrogenase (LDH) release in SH-SY5Y cells and in LLC-PK1 cells (1 μM)[1]. YM-244769 possesses reverse mode-selectivity[1]. YM-244769 (1 and 10 μM) inhibits NCX current (INCX) in a concentration- and [Na+]i-dependent manner, the IC50 against the unidirectional outward INCX (Ca2+ entry mode) is 0.05 μM. The IC50 values against the bidirectional outward and inward INCX are similar and approximately 100 nM with a Hill coefficient of about 1[3]. YM-244769 is trypsin-insensitive[3]. |
| In Vivo | YM-244769 (0.1-1 mg/kg; p.o.; once) exhibits dose-dependently natriuretic action in mice and significantly increased urinary excretion of Ca2+ as well as Ca2+/Cr ratio[2]. 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. |
| References |
| Molecular Formula | C26H24Cl2FN3O3 |
|---|---|
| Molecular Weight | 516.39100 |
| Exact Mass | 515.11800 |
| PSA | 89.96000 |
| LogP | 7.86420 |
- Shanghai Nianxing Industrial Co., Ltd
- China
- Product Name: YM 244769
- Price: Negotiable
- Purity: 98.0%
- Delivery: 10 Day
- Contact: Huang
- Email: sales@echemcloud.com
- DC Chemicals Limited
- China
- Product Name: YM-244769 hydrochloride
- Price: ￥Inquiry/100mg ￥Inquiry/250mg ￥Inquiry/1g
- Purity: 98.0%
- Delivery: 10 Day
- Contact: Tony Cao
- Email: sales@dcchemicals.com
- Dayang Chem (Hangzhou) Co., Ltd.
- China
- Product Name: YM 2447690
- Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
- Purity: 98.0%
- Delivery: Inquiry
- Contact: Ms Wang
- Email: enquiry@dycnchem.com
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