ONO-RS-411
N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)benzamide hemihydrate
CAS: 150821-03-7
Molecular Formula: C27H25N5O5
ONO-RS-411 - Names and Identifiers
| Name | N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)benzamide hemihydrate |
| Synonyms | Onon Ultair RS-411 Ono-1078 SB-205312 Ono-RS-411 Pranlukast hydrate PRANLUKASTHEMIHYDRATE Ono-1070(monoNa salt) Pranlukast Hemihydrate N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phe... 8-[4(4-phenylbutoxy)benzoyl]amino-2-(5-tetrazolyl)-4-oxo-4H-1-benzopyran N-[4-oxo-2-(2H-tetrazol-5-yl)chromen-8-yl]-4-(4-phenylbutoxy)benzamide,hydrate N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)benzamide hemihydrate N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)-benzamide hemihydrate |
| CAS | 150821-03-7 |
| InChI | InChI=1/2C27H23N5O4.H2O/c2*33-23-17-24(26-29-31-32-30-26)36-25-21(23)10-6-11-22(25)28-27(34)19-12-14-20(15-13-19)35-16-5-4-9-18-7-2-1-3-8-18;/h2*1-3,6-8,10-15,17H,4-5,9,16H2,(H,28,34)(H,29,30,31,32);1H2 |
ONO-RS-411 - Physico-chemical Properties
| Molecular Formula | C27H25N5O5 |
| Molar Mass | 499.53 |
| Solubility | DMSO: ≥10mg/mL |
| Appearance | white solid |
| Storage Condition | -20°C |
| In vitro study | In the radioligand binding assay, Pranlukast (ONO-1078) inhibits [ 3 H]LTE 4 , [ 3 H]LTD 4 , and [ 3 H]LTC 4 bindings to lung membranes with K i s of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively. The antagonism of Pranlukast against [ 3 H]LTD 4 binding is competitive. In functional experiments, Pranlukast shows competitive antagonism against the LTC 4 - and LTD 4 -induced contractions of guinea pig trachea and lung parenchymal strips with a pA 2 range of 7.70 to 10.71. In the presence of an inhibitor of the bioconversion of LTC 4 to LTD 4 , Pranlukast also antagonizes the LTC 4 -induced contraction of guinea pig trachea (pA 2 =7.78). Pranlukast significantly reverses the LTD 4 -induced prolonged contraction without effect on the KCl- and BaCl 2 -induced contractions of guinea pig trachea. Oxygen-glucose deprivation (OGD)-induced nuclear translocation of CysLT 1 receptors is inhibited by pretreatment with the CysLT 1 receptor antagonist Pranlukast (10 μM). Pranlukast protects endothelial cells against ischemia-like injury. The effects of the CysLT 1 receptor antagonist Pranlukast and the 5-lipoxygenase inhibitor Zileuton on translocation are also assessed. The results show that Pranlukast, but not Zileuton, inhibits the translocation of the CysLT 1 receptor 6 h after OGD. |
| In vivo study | Carrageenan (CAR, 5 mg per mouse) is injected i.p. 24 h before LPS (50 p,g per mouse) is injected i.v. Various doses of Pranlukast (ONO-1078; 40, 20, and 10 mmol/kg), AA-861 (20, 10, and 5 mmol/kg), Indomethacin (40 mmollkg), and the controls are injected s.c. into mice 30 min before they are challenged with 50 p,g of LPS. The maximum soluble doses are 0.6 mmol/mL in 10% DMSO for AA-861 and 1.2 mmol/mL in 10% ethanol for Pranlukast. These solutions are used as the maximum doses for the treatments. The mortality of mice is significantly decreased in AA-861- Pranlukast-treated mice relative to that in the control mice. Pretreatment with CAR (5 mg i.p.) renders the mice more sensitive to the effect of LPS. Although the survival rate of mice treated with each solvent is 20% at 72 h after LPS (50 p,g per mouse) administration, s.c. treatment with AA-861 (20 mmol/kg) or Pranlukast (40 mmol/kg) significantly increases the survival rate after the LPS administration (AA-861, P<0.001; Pranlukast, P<0.01). |
ONO-RS-411 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36/37/38 - 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 |
| Hazard Class | IRRITANT |
ONO-RS-411 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.019 ml | 5.097 ml | 10.193 ml |
| 5 mM | 0.204 ml | 1.019 ml | 2.039 ml |
| 10 mM | 0.102 ml | 0.51 ml | 1.019 ml |
| 5 mM | 0.02 ml | 0.102 ml | 0.204 ml |
Last Update：2024-01-02 23:10:35
ONO-RS-411 - Reference Information
| biological activity | Pranlukast hemihydrate (ONO-1078 hemihydrate) is an efficient and competitive selective leukotriene antagonist. Pranlukast inhibited the binding of [3H]LTE4,[3H]LTD4 and [3H]LTC4 to the pulmonary membrane with Ki of 0.63±0.11,0.99±0.19 and 5640±680 nM, respectively. |
| target | LTE 4 0.63 nM (Ki) LTD 4 0.99 nM (Ki) LTC 4 5640 nM (Ki) |
| in vitro study | in the radioligand binding say, Pranlukast (ONO-1078) inhibits [ 3 H]LTE 4 , [ 3 H]LTD 4 , and [ 3 H]LTC 4 bindings to lung membranes with K I s of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively. The antagonism of Pranlukast against [ 3 H]LTD 4 binding is competitive. In functional experiments, Pranlukast shows competitive antagonism against the LTC 4 - and LTD 4 -induced contractions of guinea pig trachea and lung parenchymal strips with a pA2 range of 7.70 to 10.71. In the presence of an inhibitor of the bioconversion of LTC 4 to LTD 4, pranlukast also antagonizes the LTC 4 -induced contraction of guinea pig trachea (pA 2=7.78). Pranlukast significantly reverses the LTD 4 -induced prolonged contraction without effect on the KCl- and BaCl 2 -induced contractions of guinea pig trachea. Oxygen-glucose deprivation (OGD)-induced nuclear translocation of CysLT 1 receptors is inhibited by pretreatment with the CysLT 1 receptor antagonist Pranlukast (10 μM). Pranlukast protects endothelial cells against ischemia-like injury. The effects of the CysLT 1 receptor antagonist Pranlukast and the 5-lipoxygenase inhibitor Zileuton on translocation are also assessed. The results show that Pranlukast, but not Zileuton, inhibits the translocation of the CysLT 1 receptor 6 h after OGD. |
| in vivo study | Carrageenan (CAR, 5 mg per mouse) is injected I. p. 24 h before LPS (50 p,g per mouse) is injected I. v. Various dos of Pranlukast (ONO-1078; 40, 20, and 10 mmol/kg), AA-861 (20, 10, and 5 mmol/kg), indomethacin (40 mmollkg), and the controls are injected s.c. into mice 30 min before they are challenged with 50 p, G of LPS. The maximum soluble doses are 0.6 mmol/mL in 10% DMSO for AA-861 and 1.2 mmol/mL in 10% ethanol for Pranlukast. These solutions are used as the maximum doses for the treatments. The mortality of mice is significantly decreased in AA-861- Pranlukast-treated mice relative to that in the control mice. Pretreatment with CAR (5 mg I. p.) renders the mice more sensitive to the effect of LPS. Although the survival rate of mice treated with each solvent is 20% at 72 h after LPS (50 p, G per mouse) administration, s.c treatment with AA-861 (20 mmol/kg) or Pranlukast (40 mmol/kg) significantly increases the survival rate after the LPS administration (AA-861, P<0.001; Pranlukast, P<0.01). |
Last Update：2024-04-09 21:01:54
Supplier List
Product Name: 8-[4(4-phenylbutoxy)benzoyl]amino-2-(5-tetrazolyl)-4-oxo-4H-1-benzopyran Visit Supplier Webpage Request for quotation
CAS: 150821-03-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 150821-03-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: 8-[4(4-phenylbutoxy)benzoyl]amino-2-(5-tetrazolyl)-4-oxo-4H-1-benzopyran Visit Supplier Webpage Request for quotation
CAS: 150821-03-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 150821-03-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History