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Constitutive Androstane Receptor

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By Targets:	Constitutive Androstane Receptor (5) Antibiotic (1) Apoptosis (7) Bacterial (4) Bcl-2 Family (1) Cytochrome P450 (1) Drug Isomer (1) Endogenous Metabolite (1) Fungal (1) Histamine Receptor (5) Isotope-Labeled Compounds (1)
By Research Areas:	Cancer (6) Endocrinology (2) Infection (1) Inflammation/Immunology (6) Metabolic Disease (4) Neurological Disease (4)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Constitutive Androstane Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111634

Epsilon-momfluorothrin	Constitutive Androstane Receptor	Cancer
Epsilon-momfluorothrin is a type I synthetic pyrethroid insecticide, activates constitutive androstane receptor (CAR), and induces hepatocellular tumors in rats .

HY-W015026

Isobutylparaben Isobutyl-P-Hydroxybenzoate	Bacterial	Inflammation/Immunology
Isobutylparaben (Isobutyl 4-hydroxybenzoate) is a constitutive androstane receptor (CAR) activator. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics .

HY-103244

CITCO 2 Publications Verification	Apoptosis	Cancer
CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC₅₀ of 49 nM over *pregnane X receptor* (PXR)*, and no activity on other nuclear receptors* .

HY-110249

CINPA1 1 Publications Verification	Constitutive Androstane Receptor	Metabolic Disease
CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC₅₀ of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function .

HY-103243

TCPOBOP 3 Publications Verification	Bcl-2 Family	Cancer
TCPOBOP is a constitutive androstane receptor (CAR) agonist that induces robust hepatocyte proliferation and hepatomegaly without any liver injury or tissue loss . TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins .

HY-155295

Z-CITCO	Constitutive Androstane Receptor Drug Isomer	Metabolic Disease
Z-CITCO is the cis isomer of CITCO (HY-103244). Z-CITCO is an agonist of constitutive androstane receptor (CAR) with an EC₅₀ value of 3.9 µM .

HY-B0349S

Meclizine-d8 Meclozine-d₈	Isotope-Labeled Compounds Histamine Receptor Apoptosis	Inflammation/Immunology
Meclizine-d₈ is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR[1][2][3].

HY-W015026R

Isobutylparaben (Standard) Isobutyl-P-Hydroxybenzoate (Standard)	Bacterial	Inflammation/Immunology
Isobutylparaben (Standard) is the analytical standard of Isobutylparaben. This product is intended for research and analytical applications. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is a constitutive androstane receptor (CAR) activator. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics .

HY-W015026S

Isobutylparaben-d4 Isobutyl 4-hydroxybenzoate-d₄	Bacterial	Inflammation/Immunology
Isobutylparaben-d₄ is the deuterium labeled Isobutylparaben[1]. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is a constitutive androstane receptor (CAR) activator. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics[2].

HY-W013854

5α-Androstan-3β-ol 3β-Hydroxy-5α-Androstane	Endogenous Metabolite	Others
5α-Androstan-3β-ol (Androstan), a saturated sterol, is a CAR (constitutive androstane receptor) inverse agonist ligand. 5α-Androstan-3β-ol (Androstan) increases the AmB-channel conductance in a concentration dependent manner .

HY-110134

S07662	Constitutive Androstane Receptor	Metabolic Disease
S07662 is a human constitutive androstane receptor (hCAR) inhibitor with an IC₅₀ of 0.7 μM. S07662 recruits the corepressor NCoR in cell-based assays and attenuate the expression of CYP2B6 mRNA in human primary hepatocytes induced by phenytoin (HY-B0448) and CITCO (HY-103244) .

HY-B0349B

Meclizine dihydrochloride monohydrate Meclozine dihydrochloride monohydrate	Histamine Receptor Apoptosis	Neurological Disease Inflammation/Immunology
Meclizine (Meclozine) dihydrochloride monohydrate, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease .

HY-B0349

Meclizine dihydrochloride 2 Publications Verification Meclozine dihydrochloride	Histamine Receptor Apoptosis	Neurological Disease Endocrinology Cancer
Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .

HY-B0349A

Meclizine Meclozine	Histamine Receptor Apoptosis	Neurological Disease Inflammation/Immunology
Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease .

HY-W040129R

Chromomycin A3 (Standard)	Bacterial Fungal Apoptosis Antibiotic	Infection Cancer
Meclizine (dihydrochloride) (Standard) is the analytical standard of Meclizine (dihydrochloride). This product is intended for research and analytical applications. Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .

HY-B0349R

Meclizine (dihydrochloride) (Standard)	Histamine Receptor Apoptosis	Neurological Disease Endocrinology Cancer
Meclizine (dihydrochloride) (Standard) is the analytical standard of Meclizine (dihydrochloride). This product is intended for research and analytical applications. Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .

HY-173033

MI-883	Constitutive Androstane Receptor Cytochrome P450	Metabolic Disease
MI-883 is the orally active agonist for **Constitutive Androstane Receptor (CAR, EC₅₀*=73 nM) and the antagonist for Pregnane X Receptor* (PXR, IC₅₀=0.1 μM). MI-883 stimulates CAR LBD assembly (EC₅₀=0.38 µM) and CAR3 variant activation (EC₅₀=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. MI-883 inhibits basal PXR activity IC₅₀=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-W040129R

Chromomycin A3 (Standard)	Microorganisms Source classification	Bacterial Fungal Apoptosis Antibiotic
Meclizine (dihydrochloride) (Standard) is the analytical standard of Meclizine (dihydrochloride). This product is intended for research and analytical applications. Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .

Cat. No.	Product Name	Chemical Structure

HY-B0349S

Meclizine-d8
Meclizine-d₈ is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR[1][2][3].

HY-W015026S

Isobutylparaben-d4
Isobutylparaben-d₄ is the deuterium labeled Isobutylparaben[1]. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is a constitutive androstane receptor (CAR) activator. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics[2].

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Constitutive Androstane Receptor

Inhibitors & Agonists

NaturalProducts

Isotope-Labeled Compounds

Natural
Products