MK-571 SODIUM SALT
MK-571 (sodium salt)
CAS: 115103-85-0
Molecular Formula: C26H26ClN2NaO3S2
MK-571 SODIUM SALT - Names and Identifiers
MK-571 SODIUM SALT - Physico-chemical Properties
| Molecular Formula | C26H26ClN2NaO3S2 |
| Molar Mass | 537.06901 |
| Solubility | DMSO: ≥ 33 mg/mL |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
| In vitro study | MK-571 (L660,711) is a potent and selective competitive inhibitor of [ 3 H]leukotriene D4 binding in guinea pig (K i value, 0.22 nM) and human (K i value, 2.1 nM) lung membranes. MK-571 is essentially inactive versus [ 3 H]LTC4 binding with IC 50 values of 23±11 μM (n=16) and 32 μM (n=1) in guinea pig and human lung, respectively. MK-571 competitively antagonizes contractions of guinea pig trachea and ileum induced by leukotriene (LT) D 4 (respective pA 2 values, 9.4 and 10.5) and LTE4 (respective pA 2 values, 9.1 and 10.4) and contractions of human trachea induced by LTD 4 (pA 2 value, 8.5). MK-571 (58 nM) antagonizes contractions of guinea pig trachea induced by LTC 4 in the absence (dose ratio=28) but not in the presence of 45 mM L-serine borate (dose ratio less than 2). MK-571 (19μM) does not block contractions of guinea pig trachea induced by histamine, acetylcholine, 5-hydroxytryptamine, PGF 2 alpha, U-44069, or PGD 2 . In the presence of atropine, mepyramine, and indomethacin, MK-571 (19 μM) inhibits a small component of the response to antigen on guinea pig trachea but completely blocked anti-IgE-induced contractions of human trachea. |
| In vivo study | MK-571 (L-660,711; i.v.) antagonizes bronchoconstriction induced in anesthetized guinea pigs by i.v. LTC 4 , LTD 4 , and LTE 4 but does not block bronchoconstriction to arachidonic acid, U-44069, 5-hydroxytryptamine, histamine, or acetylcholine. Intraduodenal MK-571 antagonizes LTD 4 (0.2-12.8 μg/kg)-induced bronchoconstriction in guinea pigs, and p.o. MK-571 blockes LTD 4 - and Ascaris-induced bronchoconstriction in conscious squirrel monkeys and ovalbumin-induced bronchoconstriction in conscious sensitized rats treated with methysergide (3 μg/kg). Hypoxia-exposed WT mice are treated with either saline or MK-571 (5 mg/kg/d or 25 mg/kg/d) for 2 more weeks while being maintain in hypoxic conditions. Saline-treated mice display all the hallmarks of PH (i.e., an increase in RVSP, Fulton index, and arterial wall thickness). However, following hypoxia, MK-571-treated mice display lower RVSP and Fulton index and a decrease in the medial thickening of small pulmonary arteries and arterioles. |
MK-571 SODIUM SALT - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37 - Wear suitable protective clothing and gloves. |
| WGK Germany | 3 |
MK-571 SODIUM SALT - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.862 ml | 9.31 ml | 18.62 ml |
| 5 mM | 0.372 ml | 1.862 ml | 3.724 ml |
| 10 mM | 0.186 ml | 0.931 ml | 1.862 ml |
| 5 mM | 0.037 ml | 0.186 ml | 0.372 ml |
Last Update：2024-01-02 23:10:35
MK-571 SODIUM SALT - Reference Information
| Biological activity | MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist. The Ki in guinea pig and human lung membranes is 0.22 and 2.1 nM respectively. |
| target | LTD 4 0.22 nM (Ki, in guinea pig lung) LTD 4 2.1 nM (Ki, in human lung) |
| in vitro study | MK-571 (L660,711) is a potent and selective competitive inhibitor of [ 3 H]leukotriene D4 binding in guinea pig (K I value, 0.22 nM) and human (K I value, 2.1 nM) lung membranes. MK-571 is essentially inactive versus [ 3 H]LTC4 binding with IC 50 values of 23±11 μ m (n = 16) and 32 μ m (n = 1) in guinea pig and human lung, respectively. MK-571 competitively antagonizes contractions of guinea pig trachea and ileum induced by leukotriene (LT) D 4 (respective pA 2 values, 9.4 and 10.5) and LTE4 (respective pA 2 values, 9.1 and 10.4) and contractions of human trachea induced by LTD 4 (pA 2 value, 8.5). MK-571 (58 nM) antagonizes contractions of guinea pig trachea induced by LTC 4 in the absence (dose ratio = 28) but not in the presence of 45 mM L-serine borate (dose ratio less than 2). MK-571 (19 μ m) does not block contractions of guinea pig trachea induced by histamine, acetylcholine, 5-hydroxytryptamine, PGF 2 alpha, U-44069, or PGD 2 . In the presence of atropine, mepyramine, and indomethacin, MK-571 (19 μM) inhibits a small component of the response to antigen on guinea pig trachea but completely blocked anti-IgE-induced contractions of human trachea. |
| in vivo studies | MK-571 (L-660,711; I. v.) antagonizes bronchoconstriction induced in anesthetized guinea pigs by I. v. LTC 4 , LTD 4 , and LTE 4 but does not block bronchoconstriction to arachidonic acid, U-44069, 5-hydroxytryptamine, histamine, or acetylcholine. Intraduodenal MK-571 antagonizes LTD 4 (0.2-12.8 μg/kg)-induced bronchoconstriction in guinea pigs, and p.o. MK-571 blockes LTD 4 - and Ascaris-induced bronchoconstriction in conscious squirrel monkeys and ovalbumin-induced bronchoconstriction in conscious sensitized rats treated with methysergide (3 μg/kg). Hypoxia-exposed WT ice are treated with either salt or MK-571 (5 mg/kg/d or 25 mg/kg/d) for 2 more weeks while being maintain in hypoxic conditions. Saline-treated display all hallmarks of PH (I. e., an increase in RVSP, Fulton index, and arterial wall thickness). However, following hypoxia, MK-571-treated mice display lower RVSP and Fulton index and a decrease in the medial thickening of small pulmonary arteries and arterioles. |
Last Update：2024-04-09 21:11:58
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Product Name: MK-571 (sodium salt) Visit Supplier Webpage Request for quotationCAS: 115103-85-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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