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50847-11-5 (Ibudilast)

1

Identification

Ibudilast Ibudilast
Name Ibudilast
Formula C14H18N2O
MW 230.31
CAS No. 50847-11-5
EINECS
Smiles O=C(C(C)C)C(C(C(C)C)=N1)=C2N1C=CC=C2
Synonyms 3-Isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine; 2-Methyl-1-[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl]-1-propanone; 2-Isopropyl-3-isobutyrylpyrazolo[1,5-a]pyridine; 1-(2-isopropylpyrazolo[1,5-a]pyridin-3-yl)-2-methylpropan-1-one
InChI InChI=1S/C14H18N2O/c1-9(2)13-12(14(17)10(3)4)11-7-5-6-8-16(11)15-13/h5-10H,1-4H3
2

Introduction

Ibudilast(KC-404;AV-411;MN-166) is a relatively nonselective phosphodiesterase inhibitor which has been marketed for treating asthma. Target: PDE Ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) is a nonselective inhibitor of cyclic nucleotide phosphodiesterase (PDE).

Background Information

Ibudilast is a potent PDE4 inhibitor for PDE4A with IC50 of 54 nM. ......by AbMole BioScience
Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency Virus-1 Tat-Mediated activation of microglial cells. ......by AdooQ BioScience, LLC
Ibudilast is a nonselective inhibitor of cyclic nucleotide phosphodiesterase (PDE) which has been marketed for treating asthma. It crosses the blood-brain barrier, is well tolerated, is active on oral administration, reduces glial activation and attenuate ......by BOC Sciences
Ibudilast is a phosphodiesterase inhibitor ......by BioVision, Inc.,
Ibudilast, also known as AV-411, KC-404 and MN-166, is an antiinflammatory drug used mainly in Japan, which acts as a phosphodiesterase inhibitor, inhibiting the PDE-4 subtype to the greatest extent, but also showing significant inhibition of other PDE subtypes. Ibudilast has bronchodilator, vasodilator and neuroprotective effects, and is mainly used in the treatment of asthma and stroke. It inhibits platelet aggregation, and may also be useful in the treatment of multiple sclerosis. ......by MedKoo Biosciences, Inc.
Ibudilast is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities. ......by Selleck Chemicals LLC
Ibudilast is an anti-inflammatory and neuroprotective oral agent which shows an excellent safety profile at 60 mg/day and provides significantly prolonged time-to-first relapse and attenuated brain volume shrinkage in patients with relapsing-remitting (RR) and/or secondary progressive (SP) multiple sclerosis (MS). Ibudilast is currently in development in the U.S. (codes: AV-411 or MN-166), but is approved for use as an antiinflammatory in Japan. ......by Target Molecule Corp.
Phosphodiesterase inhibitor (IC50 values are 53, 35, 48, 12 and 10 μM for PDE Ia, II, III, IV and V respectively). Inhibits platelet aggregation and is an orally-active cerebral vasodilator, bronchodilator and antiallergic agent. ......by Tocris Bioscience Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000011550

Storage condition

Store at RT by Tocris Bioscience Inc.

Solubility

DMSO by MedChemexpress Co., Ltd.
Soluble to 100 mM in DMSO and to 100 mM in ethanol by Tocris Bioscience Inc.
5

Mechanism and Indication

Signaling Pathways Metabolic Enzyme/Protease
Target Phosphodiesterase (PDE)
Research Area Inflammation/Immunology
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Ibudilast - Launched
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Safety Data of Ibudilast

Hazard Symbols : Xn
Risk Statements : R22;R36/37/38
Safety Statements : S26;S36
RTECS : UR0711200
WGKGermany : 3
8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience USA
AdooQ BioScience, LLC USA
Alfa Chemistry USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
Beijing Huikang Boyuan Chemical Tech Co., Ltd. China
BioVision, Inc., USA
Biochempartner Co., Ltd China
Bosche Scientific LLC, USA
CHEMSCENE, LLC 10mg/USD42();50mg/USD59() USA
Cayman Chemical Company USA
MedChemexpress Co., Ltd. 10mg/USD42();50mg/USD59() USA
MedKoo Biosciences, Inc. USA
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD42();50mg/USD59() China
Target Molecule Corp. 1mg/USD47();10mg/USD168();25mg/USD288();50mg/USD488() USA
Tocris Bioscience Inc. USA
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Related Products

Other Forms of 50847-11-5

Name CAS No Formula MW

Recommended Compounds in Phosphodiesterase (PDE)

Name CAS No Formula MW
(R)-(-)-Rolipram 85416-75-7 C16H21NO3 275.34
Mirodenafil (dihydrochloride) 862189-96-6 C26H39Cl2N5O5S 604.59
Vardenafil (hydrochloride) 224785-91-5 C23H33ClN6O4S 525.06
Pentoxifylline 6493-05-6 C13H18N4O3 278.31
Anagrelide (hydrochloride) 58579-51-4 C10H8Cl3N3O 292.55
Vardenafil 224785-90-4 C23H32N6O4S 488.6
(S)-(+)-Rolipram 85416-73-5 C16H21NO3 275.34
Irsogladine (maleate) 84504-69-8 C13H11Cl2N5O4 372.16
Irsogladine 57381-26-7 C9H7Cl2N5 256.09
Dipyridamole (hydrochloride)(1:x) 35763-39-4 C24H41ClN8O4 541.09
Dipyridamole 58-32-2 C24H40N8O4 504.63
Pimobendan (hydrochloride) 77469-98-8 C19H19ClN4O2 370.83
Pimobendan 74150-27-9 C19H18N4O2 334.37
Aminophylline 317-34-0 C16H24N10O4 420.43
Diphylline 479-18-5 C10H14N4O4 254.24
Cilostazol 73963-72-1 C20H27N5O2 369.46
Deltarasin (hydrochloride) 1440898-82-7 C40H38ClN5O 640.22
Rolipram 61413-54-5 C16H21NO3 275.34
Deltarasin 1440898-61-2 C40H37N5O 603.75
Sildenafil (citrate) 171599-83-0 C28H38N6O11S 666.7

Recommended Compounds in Same Indication

Name CAS No Formula MW
11

Route of Synthesis

12

References

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More Information

Ibudilast

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