JTE-907 | CAS#282089-49-0 | CB2 inverse agonist

JTE-907
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 530625

CAS#: 282089-49-0

Description: JTE-907 is a drug used in scientific research that acts as a selective CB2 inverse agonist. It has antiinflammatory effects in animal studies,thought to be mediated by an interaction between the CB2 receptor and IgE.

Chemical Structure

JTE-907

CAS# 282089-49-0

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 530625
Name: JTE-907
CAS#: 282089-49-0
Chemical Formula: C24H26N2O6
Exact Mass: 438.18
Molecular Weight: 438.480
Elemental Analysis: C, 65.74; H, 5.98; N, 6.39; O, 21.89

Price and Availability

Size	Price	Availability
5mg	USD 350	2 Weeks
10mg	USD 600	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: JTE-907; JTE 907; JTE907.

IUPAC/Chemical Name: N-(1,3-benzodioxol-5-ylmethyl)-1,2-dihydro-7-methoxy-2-oxo-8-(pentyloxy)-3-Quinolinecarboxamide

InChi Key: GRAJFFFXJYFVOC-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H26N2O6/c1-3-4-5-10-30-22-19(29-2)9-7-16-12-17(24(28)26-21(16)22)23(27)25-13-15-6-8-18-20(11-15)32-14-31-18/h6-9,11-12H,3-5,10,13-14H2,1-2H3,(H,25,27)(H,26,28)

SMILES Code: O=C(C1=CC2=C(NC1=O)C(OCCCCC)=C(OC)C=C2)NCC3=CC=C(OCO4)C4=C3

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:	JTE-907 is a highly selective, orally active CB2 receptor inverse agonist and exerts anti-inflammatory effects in vivo.
In vitro activity:	JTE-907 (10, but not 1, mg/kg) and tacrolimus, but not betamethasone, tended to alleviate the dermatitis. Betamethasone inhibited the body weight gain. These results suggest that JTE-907 suppresses spontaneous itch-associated responses of NC mice without adverse effects such as weight loss. Reference: Eur J Pharmacol. 2006 Aug 7;542(1-3):179-83. https://pubmed.ncbi.nlm.nih.gov/16824511/
In vivo activity:	Transient administration of the cannabinoid receptor 2 antagonist AM630 (10 mg/kg) or inverse agonist JTE907 (3 mg/kg) during immunization heightens the intensity and breadth of antigen-specific immune responses in young and aged mice through the upregulation of immunomodulatory genes in secondary lymphoid tissues. Reference: Sci Rep. 2017 Feb 17;7:42584. https://pubmed.ncbi.nlm.nih.gov/28209996/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	16.6	37.86
	DMF:PBS (pH 7.2) (1:2)	0.2	0.46
	DMSO	56.3	128.48
	Ethanol	4.4	10.00
	Methanol	1.0	2.28

Preparing Stock Solutions

The following data is based on the product molecular weight 438.48 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. Ruz-Maldonado I, Atanes P, Huang GC, Liu B, Persaud SJ. Direct Stimulatory Effects of the CB2 Ligand JTE 907 in Human and Mouse Islets. Cells. 2021 Mar 22;10(3):700. doi: 10.3390/cells10030700. PMID: 33809893; PMCID: PMC8004177. 2. Maekawa T, Nojima H, Kuraishi Y, Aisaka K. The cannabinoid CB2 receptor inverse agonist JTE-907 suppresses spontaneous itch-associated responses of NC mice, a model of atopic dermatitis. Eur J Pharmacol. 2006 Aug 7;542(1-3):179-83. doi: 10.1016/j.ejphar.2006.05.040. Epub 2006 Jun 2. PMID: 16824511. 3. Dotsey E, Ushach I, Pone E, Nakajima R, Jasinskas A, Argueta DA, Dillon A, DiPatrizio N, Davies H, Zlotnik A, Crompton PD, Felgner PL. Transient Cannabinoid Receptor 2 Blockade during Immunization Heightens Intensity and Breadth of Antigen-specific Antibody Responses in Young and Aged mice. Sci Rep. 2017 Feb 17;7:42584. doi: 10.1038/srep42584. PMID: 28209996; PMCID: PMC5314369. 4. Ueda Y, Miyagawa N, Matsui T, Kaya T, Iwamura H. Involvement of cannabinoid CB(2) receptor-mediated response and efficacy of cannabinoid CB(2) receptor inverse agonist, JTE-907, in cutaneous inflammation in mice. Eur J Pharmacol. 2005 Sep 27;520(1-3):164-71. doi: 10.1016/j.ejphar.2005.08.013. PMID: 16153638.
In vitro protocol:	1. Ruz-Maldonado I, Atanes P, Huang GC, Liu B, Persaud SJ. Direct Stimulatory Effects of the CB2 Ligand JTE 907 in Human and Mouse Islets. Cells. 2021 Mar 22;10(3):700. doi: 10.3390/cells10030700. PMID: 33809893; PMCID: PMC8004177. 2. Maekawa T, Nojima H, Kuraishi Y, Aisaka K. The cannabinoid CB2 receptor inverse agonist JTE-907 suppresses spontaneous itch-associated responses of NC mice, a model of atopic dermatitis. Eur J Pharmacol. 2006 Aug 7;542(1-3):179-83. doi: 10.1016/j.ejphar.2006.05.040. Epub 2006 Jun 2. PMID: 16824511.
In vivo protocol:	1. Dotsey E, Ushach I, Pone E, Nakajima R, Jasinskas A, Argueta DA, Dillon A, DiPatrizio N, Davies H, Zlotnik A, Crompton PD, Felgner PL. Transient Cannabinoid Receptor 2 Blockade during Immunization Heightens Intensity and Breadth of Antigen-specific Antibody Responses in Young and Aged mice. Sci Rep. 2017 Feb 17;7:42584. doi: 10.1038/srep42584. PMID: 28209996; PMCID: PMC5314369. 2. Ueda Y, Miyagawa N, Matsui T, Kaya T, Iwamura H. Involvement of cannabinoid CB(2) receptor-mediated response and efficacy of cannabinoid CB(2) receptor inverse agonist, JTE-907, in cutaneous inflammation in mice. Eur J Pharmacol. 2005 Sep 27;520(1-3):164-71. doi: 10.1016/j.ejphar.2005.08.013. PMID: 16153638.

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1: Altun A, Yildirim K, Ozdemir E, Bagcivan I, Gursoy S, Durmus N. Attenuation of morphine antinociceptive tolerance by cannabinoid CB1 and CB2 receptor antagonists. J Physiol Sci. 2015 Sep;65(5):407-15. doi: 10.1007/s12576-015-0379-2. Epub 2015 Apr 18. PubMed PMID: 25894754.

2: Marini P, Cascio MG, King A, Pertwee RG, Ross RA. Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors. Br J Pharmacol. 2013 Jun;169(4):887-99. doi: 10.1111/bph.12191. PubMed PMID: 23711022; PubMed Central PMCID: PMC3687668.

3: Harvey BS, Nicotra LL, Vu M, Smid SD. Cannabinoid CB2 receptor activation attenuates cytokine-evoked mucosal damage in a human colonic explant model without changing epithelial permeability. Cytokine. 2013 Aug;63(2):209-17. doi: 10.1016/j.cyto.2013.04.032. Epub 2013 May 22. PubMed PMID: 23706402.

4: Franklin JM, Vasiljevik T, Prisinzano TE, Carrasco GA. Cannabinoid agonists increase the interaction between β-Arrestin 2 and ERK1/2 and upregulate β-Arrestin 2 and 5-HT(2A) receptors. Pharmacol Res. 2013 Feb;68(1):46-58. doi: 10.1016/j.phrs.2012.11.002. Epub 2012 Nov 19. PubMed PMID: 23174265; PubMed Central PMCID: PMC3562593.

5: González-Muniesa P, Bing C, Trayhurn P. Upregulation of the expression of inflammatory and angiogenic markers in human adipocytes by a synthetic cannabinoid, JTE-907. Horm Metab Res. 2010 Sep;42(10):710-7. doi: 10.1055/s-0030-1255119. Epub 2010 Jul 5. PubMed PMID: 20603779.

6: Morgan NH, Stanford IM, Woodhall GL. Functional CB2 type cannabinoid receptors at CNS synapses. Neuropharmacology. 2009 Sep;57(4):356-68. doi: 10.1016/j.neuropharm.2009.07.017. Epub 2009 Jul 16. PubMed PMID: 19616018.

7: Smid SD, Bjorklund CK, Svensson KM, Heigis S, Revesz A. The endocannabinoids anandamide and 2-arachidonoylglycerol inhibit cholinergic contractility in the human colon. Eur J Pharmacol. 2007 Dec 1;575(1-3):168-76. Epub 2007 Jul 26. PubMed PMID: 17706636.

8: Ueda Y, Miyagawa N, Wakitani K. Involvement of cannabinoid CB2 receptors in the IgE-mediated triphasic cutaneous reaction in mice. Life Sci. 2007 Jan 9;80(5):414-9. Epub 2006 Sep 30. PubMed PMID: 17055000.

9: Maekawa T, Nojima H, Kuraishi Y, Aisaka K. The cannabinoid CB2 receptor inverse agonist JTE-907 suppresses spontaneous itch-associated responses of NC mice, a model of atopic dermatitis. Eur J Pharmacol. 2006 Aug 7;542(1-3):179-83. Epub 2006 Jun 2. PubMed PMID: 16824511.

10: Raitio KH, Savinainen JR, Vepsäläinen J, Laitinen JT, Poso A, Järvinen T, Nevalainen T. Synthesis and SAR studies of 2-oxoquinoline derivatives as CB2 receptor inverse agonists. J Med Chem. 2006 Mar 23;49(6):2022-7. PubMed PMID: 16539390.

11: Ueda Y, Miyagawa N, Matsui T, Kaya T, Iwamura H. Involvement of cannabinoid CB(2) receptor-mediated response and efficacy of cannabinoid CB(2) receptor inverse agonist, JTE-907, in cutaneous inflammation in mice. Eur J Pharmacol. 2005 Sep 27;520(1-3):164-71. PubMed PMID: 16153638.

12: Iwamura H, Suzuki H, Ueda Y, Kaya T, Inaba T. In vitro and in vivo pharmacological characterization of JTE-907, a novel selective ligand for cannabinoid CB2 receptor. J Pharmacol Exp Ther. 2001 Feb;296(2):420-5. PubMed PMID: 11160626.

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