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URB597 FAAH inhibitor

Name: URB597
Brand: Selleck Chemicals
SKU: S2631
Availability: InStock
Rating: 5 (8 reviews)

Cat.No.S2631

URB597 (KDS-4103) is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets. Phase 1.

Chemical Structure

Molecular Weight: 338.4

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S263101 DMSO]68 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.73%

99.73

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS ROR
Related Products	Biochanin A PF-3845 JNJ-42165279 PF-04457845

Chemical Information, Storage & Stability

Molecular Weight	338.4	Formula	C₂₀H₂₂N₂O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	546141-08-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	KDS-4103			Smiles	C1CCC(CC1)NC(=O)OC2=CC=CC(=C2)C3=CC(=CC=C3)C(=O)N

Solubility

In vitro
Batch:

DMSO : 68 mg/mL ( (200.94 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (2.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	FAAH ^[1] 4.6 nM
In vitro	URB597 binds in the hydrophobic pocket and catalytic core of FAAH that connects the active site residues to the membrane surface of FAAH. ^[1] This compound inhibits FAAH activity in human liver microsomes with IC50 of 3 nM. ^[2] It reduces the expression of the LPS-induced enzymes cyclo-oxygenase 2 (COX-2) and inducible nitric oxide synthase (iNOS; NOS2) in primary rat microglial cell, with a concomitant reduction in the release of the inflammatory mediators prostaglandin E2 (PGE2) and (NO) nitric oxide. ^[3] This chemical evokes Ca₂₊ entry in HEK293-F Cells transiently expressing human or rat TRPA1 gene. It also activates Ca₂₊ entry in rat DRG neurons natively expressed TRPA1 channels. ^[4]
In vivo	URB597 inhibits [³H]anandamide hydrolysis in rat brain membranes with a parallel increase in brain anandamide, OEA, and PEA content by inhibition of FAAH. This compound enhances the hypothermia effect induced by ethanolamide by inhibiting FAAH. ^[5] When delivered intraperitonealy (0.3 mg/kg) it reduces allodynia and hyperalgesia through cannabinoid CB1 and CB2 receptor-mediated analgesia in rats with inflammatory pain. ^[6] This chemical reduces the reduction in body weight gain and sucrose intake induced by the chronic mild stress in rats through inhibition of brain FAAH activity. ^[7] It could reverse most depressive-like symptoms induced by adolescent THC exposure in femal rats. ^[8]
References	https://pubmed.ncbi.nlm.nih.gov/15456244/ https://pubmed.ncbi.nlm.nih.gov/16834756/ https://pubmed.ncbi.nlm.nih.gov/17543306/ https://pubmed.ncbi.nlm.nih.gov/17314320/ https://pubmed.ncbi.nlm.nih.gov/15579492/ https://pubmed.ncbi.nlm.nih.gov/16331291/ https://pubmed.ncbi.nlm.nih.gov/17511970/ https://pubmed.ncbi.nlm.nih.gov/20850463/

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