JNJ-1661010 | CAS#681136-29-8 | FAAH Inhibitor

JNJ-1661010
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525305

CAS#: 681136-29-8

Description: JNJ-1661010 is a selective, reversible inhibitor of fatty acid amide hydrolase (FAAH) (IC50 = 12 nM). JNJ-1661010 is a brain penetrant and active in vivo.

Chemical Structure

JNJ-1661010

CAS# 681136-29-8

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 525305
Name: JNJ-1661010
CAS#: 681136-29-8
Chemical Formula: C19H19N5OS
Exact Mass: 365.13
Molecular Weight: 365.455
Elemental Analysis: C, 62.44; H, 5.24; N, 19.16; O, 4.38; S, 8.77

Price and Availability

Size	Price	Availability
10mg	USD 285	2 Weeks
25mg	USD 550	2 Weeks
50mg	USD 850	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: JNJ-1661010; JNJ 1661010; JNJ1661010.

IUPAC/Chemical Name: 1-Piperazinecarboxamide, N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)-

InChi Key: BHBOSTKQCZEAJM-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H19N5OS/c25-18(20-16-9-5-2-6-10-16)23-11-13-24(14-12-23)19-21-17(22-26-19)15-7-3-1-4-8-15/h1-10H,11-14H2,(H,20,25)

SMILES Code: O=C(N1CCN(C2=NC(C3=CC=CC=C3)=NS2)CC1)NC4=CC=CC=C4

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	JNJ-1661010 (Takeda-25) a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 34 and 33 nM for rat FAAH and human FAAH, respectively.
In vitro activity:	Under these conditions, AEA (at 10−6 M and 10−8 M) and concomitant FAAH inhibition with JNJ1661010 (1 μM) reduced the production of IL-6 and IL-8 by RA but not OA mixed synoviocytes (Fig. 1b, d). Reference: Arthritis Res Ther. 2015 Nov 14;17:321. https://pubmed.ncbi.nlm.nih.gov/26567045/
In vivo activity:	JNJ-1661010 dose-dependently increases arachidonoyl ethanolamide, oleoyl ethanolamide, and palmitoyl ethanolamide in the rat brain. The compound attenuates tactile allodynia in the rat mild thermal injury model of acute tissue damage and in the rat spinal nerve ligation (Chung) model of neuropathic pain. JNJ-1661010 also diminishes thermal hyperalgesia in the inflammatory rat carrageenan paw model. These data suggest that FAAH inhibitors with modes of action similar to JNJ-1661010 may be useful clinically as broad-spectrum analgesics. Reference: Anesth Analg. 2009 Jan;108(1):316-29. https://pubmed.ncbi.nlm.nih.gov/19095868/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	25.0	68.41
	DMF:PBS (pH 7.2) (1:5)	0.2	0.44
	DMSO	48.1	131.72
	Ethanol	2.6	7.05

Preparing Stock Solutions

The following data is based on the product molecular weight 365.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Lowin T, Apitz M, Anders S, Straub RH. Anti-inflammatory effects of N-acylethanolamines in rheumatoid arthritis synovial cells are mediated by TRPV1 and TRPA1 in a COX-2 dependent manner. Arthritis Res Ther. 2015 Nov 14;17:321. doi: 10.1186/s13075-015-0845-5. PMID: 26567045; PMCID: PMC4644337. 2. Karbarz MJ, Luo L, Chang L, Tham CS, Palmer JA, Wilson SJ, Wennerholm ML, Brown SM, Scott BP, Apodaca RL, Keith JM, Wu J, Breitenbucher JG, Chaplan SR, Webb M. Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth Analg. 2009 Jan;108(1):316-29. doi: 10.1213/ane.0b013e31818c7cbd. PMID: 19095868.
In vitro protocol:	1. Lowin T, Apitz M, Anders S, Straub RH. Anti-inflammatory effects of N-acylethanolamines in rheumatoid arthritis synovial cells are mediated by TRPV1 and TRPA1 in a COX-2 dependent manner. Arthritis Res Ther. 2015 Nov 14;17:321. doi: 10.1186/s13075-015-0845-5. PMID: 26567045; PMCID: PMC4644337. 2. Karbarz MJ, Luo L, Chang L, Tham CS, Palmer JA, Wilson SJ, Wennerholm ML, Brown SM, Scott BP, Apodaca RL, Keith JM, Wu J, Breitenbucher JG, Chaplan SR, Webb M. Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth Analg. 2009 Jan;108(1):316-29. doi: 10.1213/ane.0b013e31818c7cbd. PMID: 19095868.
In vivo protocol:	1. Lowin T, Apitz M, Anders S, Straub RH. Anti-inflammatory effects of N-acylethanolamines in rheumatoid arthritis synovial cells are mediated by TRPV1 and TRPA1 in a COX-2 dependent manner. Arthritis Res Ther. 2015 Nov 14;17:321. doi: 10.1186/s13075-015-0845-5. PMID: 26567045; PMCID: PMC4644337. 2. Karbarz MJ, Luo L, Chang L, Tham CS, Palmer JA, Wilson SJ, Wennerholm ML, Brown SM, Scott BP, Apodaca RL, Keith JM, Wu J, Breitenbucher JG, Chaplan SR, Webb M. Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth Analg. 2009 Jan;108(1):316-29. doi: 10.1213/ane.0b013e31818c7cbd. PMID: 19095868.

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1: Karbarz MJ, Luo L, Chang L, Tham CS, Palmer JA, Wilson SJ, Wennerholm ML, Brown SM, Scott BP, Apodaca RL, Keith JM, Wu J, Breitenbucher JG, Chaplan SR, Webb M. Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth Analg. 2009 Jan;108(1):316-29. doi: 10.1213/ane.0b013e31818c7cbd. PubMed PMID: 19095868.

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