BAY-u9773 (CAS 154978-38-8) || Cayman Chemical

BAY-u9773

Cayman Chemical Item Number 70770

(CAS 154978-38-8)

BAY-u9773 (CAS 154978-38-8)

Description

The biological effects of the cysteinyl leukotrienes (cysLTs, including LTC₄, LTD₄, and LTE₄) are transduced mainly by a pair of 7-transmembrane receptors, CysLT₁ and CysLT₂.^1,2,3 BAY-u9773 is a non-selective antagonist of the CysLT receptors, having about the same IC₅₀ (20-80 nM) for the inhibition of LT responses in a variety of tissue preparations containing either/or both receptors.⁴ In contrast, many of the commercially developed CysLT₁ receptor antagonists (pranlukast or montelukast) antagonize only CysLT₁ receptors. BAY-u9773 is thus one of the only available tools for blocking CysLT₂ receptors.

1 Lynch, K.R., O'Neill, G.P., Liu, Q., et al. Characterization of the human cysteinyl leukotriene CysLT₁ receptor. Nature 399 789-793 (1999).

2 Heise, C.E., O'Dowd, B.F., Figueroa, D.J., et al. Characterization of the human cysteinyl leukotriene 2 receptor. J Biol Chem 275 30531-30536 (2000).

3 Ogasawara, H., Ishii, S., Yokomizo, T., et al. Characterization of mouse cysteinyl leukotriene receptors mCysLT1 and mCysLT2. Differential pharmacological properties and tissue distribution. J Biol Chem 277(21) 18763-18768 (2002).

4 Tudhope, S.R., Cuthbert, N.J., Abram, T.S., et al. BAY u9773, a novel antagonist of cysteinyl-leukotrienes with activity against two receptor subtypes. Eur J Pharmacol 264 317-323 (1994).

Formal Name

4-[[(1R,2E,4E,6Z,9Z)-1-[(1S)-4-carboxy-1-hydroxybutyl]-2,4,6,9-pentadecatetraenyl]thio]-benzoic acid

CAS Number

154978-38-8

Molecular Formula

C₂₇H₃₆O₅S

Formula Weight

472.6

Formulation

A solution in ethanol

Purity

>95%

λ_max

279 nm

Stability

1 year

Storage

-80°C

Shipping

Dry ice in continental US; may vary elsewhere

SMILES

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CCCCC/C=C\C\C=C/C=C\C=C/[C@@H](Sc1ccc(cc1)C(=O)O)C(O)CCCC(=O)O

Background Reading

Ogasawara, H., Ishii, S., Yokomizo, T., et al. Characterization of mouse cysteinyl leukotriene receptors mCysLT1 and mCysLT2. Differential pharmacological properties and tissue distribution. J Biol Chem 277(21) 18763-18768 (2002).

Tudhope, S.R., Cuthbert, N.J., Abram, T.S., et al. BAY u9773, a novel antagonist of cysteinyl-leukotrienes with activity against two receptor subtypes. Eur J Pharmacol 264 317-323 (1994).

Heise, C.E., O'Dowd, B.F., Figueroa, D.J., et al. Characterization of the human cysteinyl leukotriene 2 receptor. J Biol Chem 275 30531-30536 (2000).

Lynch, K.R., O'Neill, G.P., Liu, Q., et al. Characterization of the human cysteinyl leukotriene CysLT₁ receptor. Nature 399 789-793 (1999).

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Size

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