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AB143333

Ibudilast, PDE inhibitor

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MW 230.31 Da, Purity >98%. Non-selective PDE inhibitor (IC50 values are 53, 35, 48, 12 and 10 μM for PDE Ia, II, III, IV and V respectively). Anti-inflammatory agent. Inhibits platelet aggregation. Centrally active via glial cell attenuation. Shows bronchodilatory, vasodilatory and neuroprotective effects in vivo. Orally active. Blood-brain barrier permeable.

View Alternative Names

5''-cyclic phosphodiesterase 4A, 5''-cyclic phosphodiesterase 4B, 5''-cyclic phosphodiesterase 4C, 5''-cyclic phosphodiesterase 4D, ACLS, CP2D6_HUMAN, CPD6, CYP2D, CYP2D7AP, CYP2D7BP, CYP2D7P2, CYP2D8P2, CYP2DL1, CYPIID6, Cholesterol 25-hydroxylase, Cytochrome P450 2D6, Cytochrome P450 family 2 subfamily D member 6, Cytochrome P450 family 2 subfamily D polypeptide 6, Cytochrome P450-DB1, DKFZp686F2182, DKFZp686M11213, DNA binding protein, DPDE 1, DPDE2, DPDE3, DPDE4, Debrisoquine 4-hydroxylase, Dunce like phosphodiesterase E3, FLJ97311, GCPS, GLI Kruppel family member GLI 3, GLI Kruppel family member GLI3 (Greig cephalopolysyndactyly syndrome), GLI family zinc finger 3, GLI3 C-terminally truncated form, GLI3 form of 190 kDa, GLI3 form of 83 kDa, GLI3 full length protein, GLI3-190, GLI3-83, GLI3FL, GLI3_HUMAN, Glioma associated oncogene family zinc finger 3, HSPDE4D, MGC126222, MGC126529, Microsomal monooxygenase, OTTHUMP00000010652, OTTHUMP00000010653, OTTHUMP00000010654, OTTHUMP00000010656, OTTHUMP00000232365, Oncogene GLI3, P450 DB1, P450C2D, PAP A, PAPB, PDE 21, PDE IVB, PDE32, PDE4, PDE43, PDE46, PDE4A11, PDE4A_HUMAN, PDE4B5, PDE4B_HUMAN, PDE4C_HUMAN, PDE4DN2, PDE4D_HUMAN, PPD IV, Phosphodiesterase 4A, Phosphodiesterase 4A, cAMP-specific (dunce, Phosphodiesterase 4B, Phosphodiesterase 4B cAMP specific, Phosphodiesterase 4B, cAMP specific (phosphodiesterase E4 dunce homolog, Drosophila), Phosphodiesterase 4C, Phosphodiesterase 4C cAMP specific, Phosphodiesterase 4C, cAMP specific (phosphodiesterase E1 dunce homolog, Drosophila), Phosphodiesterase 4D cAMP specific (dunce (Drosophila) homolog phosphodiesterase E3), Phosphodiesterase 4D cAMP specific (phosphodiesterase E3 dunce homolog Drosophila), Phosphodiesterase 4D cAMP-specific, Phosphodiesterase 4D, cAMP specific (dunce), Phosphodiesterase E1 dunce homolog, Phosphodiesterase E1 dunce homolog Drosophila, Phosphodiesterase E2 dunce homolog, Drosophila, Phosphodiesterase type 4C, STRK1, Transcriptional activator GLI3, Transcriptional repressor GLI3R, Xenobiotic monooxygenase, Zinc finger protein GLI 3, cAMP specific 3' 5' cyclic phosphodiesterase 4C, cAMP specific 3',5' cyclic phosphodiesterase 4D, cAMP specific phosphodiesterase, cAMP specific phosphodiesterase 4D, cAMP specific phosphodiesterase PDE4D6, cAMP-specific 3'', cAMP-specific 3',5'-cyclic phosphodiesterase 4A, cAMP-specific 3',5'-cyclic phosphodiesterase 4B, cAMP-specific phosphodiesterase-4 B isoform, dunce like phosphodiesterase E2, dunce-like phosphodiesterase E4, flavoprotein-linked monooxygenase, phosphodiesterase 4A cAMP specific, phosphodiesterase E2 dunce homolog, phosphodiesterase isozyme 4, phosphodiesterase type 4A11

1 Images
Chemical Structure - Ibudilast, PDE inhibitor (AB143333)
  • Chemical Structure

Lab

Chemical Structure - Ibudilast, PDE inhibitor (AB143333)

2D chemical structure image of ab143333, Ibudilast, PDE inhibitor

Key facts

CAS number

50847-11-5

Purity

>98%

Molecular weight

230.31 Da

Molecular formula

C<sub>1</sub><sub>4</sub>H<sub>1</sub><sub>8</sub>N<sub>2</sub>O

PubChem

3671

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Soluble in ethanol to 100 mM

Biochemical name

Ibudilast

Biological description

Non-selective PDE inhibitor (IC50 values are 53, 35, 48, 12 and 10 μM for PDE Ia, II, III, IV and V respectively). Anti-inflammatory agent. Inhibits platelet aggregation. Centrally active via glial cell attenuation. Shows bronchodilatory, vasodilatory and neuroprotective effects in vivo. Orally active. Blood-brain barrier permeable.

Canonical smiles

CC(C)C1=NN2C=CC=CC2=C1C(=O)C(C)C

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

InChiKey

ZJVFLBOZORBYFE-UHFFFAOYSA-N

IUPAC Name

2-methyl-1-(2-propan-2-ylpyrazolo[1,5-a]pyridin-3-yl)propan-1-one

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate long-term storage conditions
Ambient
Storage information
The product can be stored for up to 12 months

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Gli3 also known as GLI family zinc finger 3 is a transcription factor with a mass of approximately 170 kDa. This protein plays an important role in regulating gene expression especially in the Hedgehog signaling pathway. Gli3 is expressed in various tissues including the brain limbs and lungs. CYP2D6 also known as Cytochrome P450 2D6 is an enzyme involved in the metabolism of many drugs. It weighs about 55 kDa and is mainly found in the liver. PDE4 isoforms including PDE4A PDE4B PDE4C and PDE4D are phosphodiesterases that degrade the cyclic AMP (cAMP) molecule. PDE4 enzymes are localized in immune cells smooth muscle and the central nervous system.
Biological function summary

Gli3 functions in gene expression regulation and limb development. It acts as a transcriptional activator or repressor depending on cellular context and interacting partners contributing to embryonic developmental processes. CYP2D6 is an important component of drug metabolism affecting the pharmacokinetics of many medications. PDE4 family members serve to modulate cellular responses to cAMP playing roles in processes such as inflammation and cognition. These phosphodiesterases are part of a larger signaling complex that prevents excessive cAMP accumulation by breaking it down essential for maintaining proper cellular signaling balance.

Pathways

Gli3 plays a role in the Hedgehog and Notch signaling pathways where it interacts with other proteins like Sonic Hedgehog (SHH) and Patched (PTCH). This involvement is important in developmental biology and pattern formation. CYP2D6 is involved in the hepatic drug metabolism pathway related closely to its cytochrome P450 family members that aid in oxidizing xenobiotic compounds. PDE4 isoforms are part of the cAMP signaling pathway modulating various cellular reactions and interacting with cyclic AMP response element-binding protein (CREB) to influence CREB-mediated transcriptional activities.

Gli3 mutations are connected to conditions such as Greig cephalopolysyndactyly syndrome and Pallister-Hall syndrome which are developmental disorders. Abnormal functioning of Gli3 links to disruption in the Hedgehog signaling pathway interacting with proteins like GLI2. CYP2D6 genetic polymorphisms impact drug efficacy and safety associated with diseases such as depression and Parkinson's disease through its enzymatic impact on drug metabolization. PDE4 inhibitors like ibudilast and caffeine are investigated for their potential in treating inflammatory and neurodegenerative disorders given PDE4's connection to inflammation through TNF-alpha regulation and neuroprotection.

Product protocols

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