| Field | Specification |
|---|---|
| Target | |
| Alternative names | YM-57158 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C32H33ClN6O5S2 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
YM158 free base, also known as YM-57158, is a potent and selective LTD4 and TXA2 receptor antagonist, with pA2 values of about 8.87 and 8.81, respectively. Its molecular formula is C32H33ClN6O5S2, with a molecular weight of 681.22 g/mol.
Physical & Chemical Properties
| CAS Number | 179102-65-9 |
|---|---|
| Molecular Formula | C32H33ClN6O5S2 |
| Molecular Weight | 681.22 g/mol |
| SMILES | O=C(NC1=CC(CCCS(=O)(C2=CC=C(Cl)C=C2)=O)=CC=C1OCC3=NN=NN3)C4=CC=CC(OCC5=NC(C(C)(C)C)=CS5)=C4 |
| Target | LTD 4 8.87 (pA2), TXA 2 Receptor 8.81 (pA2) |
| Signaling Pathway | GPCR/G Protein |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
LTD4 8.87 (pA2) |
TXA2 Receptor 8.81 (pA2) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
Antagonism of leukotriene (LT) D4 and thromboxane (TX) A2 receptors is the action of YM158. In vitro functional assays on isolated guinea pig tracheae show YM158 acting as a competitive dual antagonist against contraction mediated by the LTD4 and TXA2 receptors, with pA2 values of about 8.87 and 8.81, respectively. Montelukast is approximately 6.5 times more potent than YM158 at the LTD4 receptor, while at the TXA2 receptor YM158 is 2.5 times more potent than Seratrodast. Tracheal contractions induced by PGD2 and PGF2α are also inhibited by YM158. In guinea pig and human platelets, YM158 antagonizes aggregation induced by U46619, a stable TXA2 analog, and it inhibits contraction of guinea pig ileum induced by LTD4. Contraction of guinea pig ileum induced by 1 nM LTD4 is inhibited by YM158 in a concentration-dependent way, giving an IC50 value of 0.58 nM[1].
In Vivo
YM158 is an orally active dual antagonist of LTD4 and TXA2 receptors and is expected to give stronger antiasthmatic efficacy than single antagonistic drugs in a broader class of asthmatic patients. YM158 is examined for its effect on these asthmatic responses in mediator-controlled and passively sensitized guinea pigs. When given p.o. 1 h before LTD4 or U46619 injection, YM158 inhibits the increase in airway resistance induced by LTD4 or U46619 in a dose-dependent manner (ED50 of 8.6 and 14 mg/kg, respectively), and p.o. YM158 exhibits antagonism of LTD4 and TXA2 receptors within the same dose range. On antigen-induced response under various conditions, oral YM158 produces significant effects of roughly the same size as the combination of Pranlukast and Daltroban: where LTD4 is predominant, where TXA2 is predominant, or where both mediators participate equally. In groups not treated with Indomethacin, YM158 (30 mg/kg), Daltroban (10 mg/kg), or a combination of Pranlukast (30 mg/kg) and Daltroban (10 mg/kg) significantly prolongs the onset time of the asthmatic response and significantly suppresses symptoms[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Animal Administration[2]
Guinea pigs[2]: Use male Hartley guinea pigs. Measure the effects of YM158 (30 mg/kg, p.o.), Pranlukast, and Daltroban on shortening of the onset time for asthmatic response. Give each compound p.o. to animals that receive no Indomethacin or Indomethacin at 5 mg/kg or 1 mg/kg[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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