1. GPCR/G Protein
  2. Leukotriene Receptor

MK-571 sodium salt (Synonyms: L-660711 sodium salt)

Cat. No.: HY-19989A Purity: 99.24%
Handling Instructions

MK-571 sodium salt is a potent, selective, orally active leukotriene receptor antagonist, which inhibits [3H] LTD4 binding in guinea pig lung with a Ki of 0.22±0.15 nM and [3H]LTD4 binding in human lung with a Ki of 2.1±1.8 nM.

For research use only. We do not sell to patients.

MK-571 sodium salt Chemical Structure

MK-571 sodium salt Chemical Structure

CAS No. : 115103-85-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 71 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
25 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 384 In-stock
Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

MK-571 sodium salt is a potent, selective, orally active leukotriene receptor antagonist, which inhibits [3H] LTD4 binding in guinea pig lung with a Ki of 0.22±0.15 nM and [3H]LTD4 binding in human lung with a Ki of 2.1±1.8 nM.

IC50 & Target[1]

LTD4

0.22 nM (Ki, In guinea pig lung)

LTD4

2.1 nM (Ki, In human lung)

In Vitro

MK-571 (L660,711) is a potent and selective competitive inhibitor of [3H]leukotriene D4 binding in guinea pig (Ki value, 0.22 nM) and human (Ki value, 2.1 nM) lung membranes. MK-571 is essentially inactive versus [3H]LTC4 binding with IC50 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) D4 (respective pA2 values, 9.4 and 10.5) and LTE4 (respective pA2 values, 9.1 and 10.4) and contractions of human trachea induced by LTD4 (pA2 value, 8.5). MK-571 (58 nM) antagonizes contractions of guinea pig trachea induced by LTC4 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, PGF2 alpha, U-44069, or PGD2. 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[1].

In Vivo

MK-571 (L-660,711; i.v.) antagonizes bronchoconstriction induced in anesthetized guinea pigs by i.v. LTC4, LTD4, and LTE4 but does not block bronchoconstriction to arachidonic acid, U-44069, 5-hydroxytryptamine, histamine, or acetylcholine. Intraduodenal MK-571 antagonizes LTD4 (0.2-12.8 μg/kg)-induced bronchoconstriction in guinea pigs, and p.o. MK-571 blockes LTD4- and Ascaris-induced bronchoconstriction in conscious squirrel monkeys and ovalbumin-induced bronchoconstriction in conscious sensitized rats treated with methysergide (3 μg/kg)[1]. 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[2].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (61.44 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8620 mL 9.3098 mL 18.6195 mL
5 mM 0.3724 mL 1.8620 mL 3.7239 mL
10 mM 0.1862 mL 0.9310 mL 1.8620 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

Mice[2]
The Mrp4-/- mice are used. Concerning the PH reversal study, 5-week-old WT mice are maintained in hypoxia for 3 weeks, then are randomized to receive, for 2 weeks, oral vehicle or MK-571 at the doses of either 5 mg/kg/d or 25 mg/kg/d. At the same time, the experiment is designed for mice in normoxia conditions. Increased hematocrit valuesare checked to assess the efficiency of hypoxia[2].

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

References
Molecular Weight

537.07

Formula

C₂₆H₂₆ClN₂NaO₃S₂

CAS No.

115103-85-0

SMILES

O=C([O-])CCSC(C1=CC=CC(/C=C/C2=NC3=CC(Cl)=CC=C3C=C2)=C1)SCCC(N(C)C)=O.[Na+]

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.24%

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Product Name:
MK-571 sodium salt
Cat. No.:
HY-19989A
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MK-571 sodium salt

Cat. No.: HY-19989A