Name | Ibudilast |
Synonyms | Ketas KC-404 Eyevinal Ibudilast IBUDILAST IBUDILAST-D7 3-Isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine 2-Isopropyl-3-isobutyrylpyrazolo[1,5-a]pyridine 1-(2-Isopropylpyrazolo[1,5-a]pyridin-3-yl)-2-methyl-1-propanone 2-methyl-1-[2-(propan-2-yl)pyrazolo[1,5-a]pyridin-3-yl]propan-1-one 2-Methyl-1-[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl]-1-propanone 1-PROPANONE, 2-METHYL-1-[2-(1-METHYLETHYL)PYRAZOLO[1,5-A]PYRIDIN-3-YL] |
CAS | 50847-11-5 |
EINECS | 637-150-7 |
InChI | InChI=1/C14H18N2O/c1-9(2)13-12(14(17)10(3)4)11-7-5-6-8-16(11)15-13/h5-10H,1-4H3 |
InChIKey | ZJVFLBOZORBYFE-UHFFFAOYSA-N |
Molecular Formula | C14H18N2O |
Molar Mass | 230.31 |
Density | 1.09 |
Melting Point | 53-54°C |
Boling Point | 175°C/7.5mmHg(lit.) |
Solubility | DMSO: 28mg/mL, soluble |
Appearance | solid |
Color | white |
Merck | 14,4879 |
pKa | 1.22±0.30(Predicted) |
Storage Condition | Sealed in dry,2-8°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
Refractive Index | 1.5500 (estimate) |
MDL | MFCD00864808 |
Physical and Chemical Properties | Colorless plate-like crystal or white crystalline powder, melting point 53.5-54 ℃ (hexane). Soluble in organic solvents, slightly soluble in water. Acute toxicity LD50 male and female mice, male and female rats (mg/kg):1880,1860,1340,1390 oral;>3000,3100,1450,1300 subcutaneous injection; 460,500,550,419 intraperitoneal injection; 160,146,43.2,42.5 intravenous injection. |
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 - Wear suitable protective clothing. |
WGK Germany | 3 |
RTECS | UR0711200 |
Toxicity | LD50 i.v. in mice: 260 mg/kg (Irikura, 1973) |
A colorless plate-like crystal or a white crystalline powder, crystallized from hexane, has a melting point of 53.5 to 54 °c. Soluble in organic solvents, slightly soluble in water.
1-amino -2-methyl pyridinium halide and isobutyric anhydride, in the presence of potassium carbonate and sodium acetate reaction, namely ibudilast.
ibudilast is a new specific Antiasthmatic agent, leukotriene receptor antagonist. For bronchial asthma, can improve the sequelae of cerebral infarction, cerebral hemorrhage sequelae and cerebral arteriosclerosis in patients with subjective symptoms.
mice were injected intravenously with LD50: 260mg/kg.
biological activity | Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities. |
Target | Value |
PDE4 (Bovine aortic EC) | 0.08 μM |
PDE2 (Bovine aortic EC) | 0.11 μM |
PDE5 (Human platelets) | 2.2 μM |
use | is used for bronchial asthma, which can improve the sequelae of cerebral infarction, sequelae of cerebral bleeding and conscious symptoms of patients with cerebral arteriosclerosis. |
Production method | 1-amino-2-methylpyridine anchor halide and isobutyric anhydride, react in the presence of potassium carbonate and sodium acetate, That is to obtain Ibustine. |