AZD1386 | CAS#942937-80-6 | TRPV1 antagonist |MedKoo

AZD-1386
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531517

CAS#: 942937-80-6 (NIH)

Description: AZD1386 is an orally available antagonist of the transient receptor potential channel TRPV1. Note: Structure of this product was from NIH/NCATS web page: https://drugs.ncats.io/drug/210323T9CP and drugbank web page: https://go.drugbank.com/drugs/DB15333.

Chemical Structure

AZD-1386

CAS# 942937-80-6 (NIH)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 531517
Name: AZD-1386
CAS#: 942937-80-6 (NIH)
Chemical Formula: C21H23F2N3O
Exact Mass: 371.18
Molecular Weight: 371.432
Elemental Analysis: C, 67.91; H, 6.24; F, 10.23; N, 11.31; O, 4.31

Price and Availability

Size	Price	Availability
5mg	USD 350	Ready to ship
10mg	USD 550	Ready to ship
25mg	USD 950	Ready to ship
50mg	USD 1650	Ready to ship
100mg	USD 2950	Ready to ship
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.

Related CAS #: 946080-23-5 942937-80-6 (NIH),

Synonym: AZD1386; AZD 1386; AZD-1386;

IUPAC/Chemical Name: 1H-Benzimidazole-1-acetamide, N-[(1S)-1-[4-(1,1-dimethylethyl)phenyl]ethyl]-6,7-difluoro-

InChi Key: FPGNKXCEPARJDI-ZDUSSCGKSA-N

InChi Code: InChI=1S/C21H23F2N3O/c1-13(14-5-7-15(8-6-14)21(2,3)4)25-18(27)11-26-12-24-17-10-9-16(22)19(23)20(17)26/h5-10,12-13H,11H2,1-4H3,(H,25,27)/t13-/m0/s1

SMILES Code: O=C(N[C@H](C1=CC=C(C(C)(C)C)C=C1)C)CN2C3=C(F)C(F)=CC=C3N=C2

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

Certificate of Analysis:

View CoA: current batch, Lot#Y23X03M12

QC Data:

View QC data: current batch, Lot#Y23X03M12

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:	AZD1386 is an orally available antagonist of the transient receptor potential channel TRPV1.
In vitro activity:	TBD
In vivo activity:	TBD

Preparing Stock Solutions

The following data is based on the product molecular weight 371.43 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:	TBD
In vitro protocol:	TBD
In vivo protocol:	TBD

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1: Quiding H, Jonzon B, Svensson O, Webster L, Reimfelt A, Karin A, Karlsten R, Segerdahl M. TRPV1 antagonistic analgesic effect: a randomized study of AZD1386 in pain after third molar extraction. Pain. 2013 Jun;154(6):808-12. doi: 10.1016/j.pain.2013.02.004. Epub 2013 Feb 19. PMID: 23541425.

2: Krarup AL, Ny L, Astrand M, Bajor A, Hvid-Jensen F, Hansen MB, Simrén M, Funch-Jensen P, Drewes AM. Randomised clinical trial: the efficacy of a transient receptor potential vanilloid 1 antagonist AZD1386 in human oesophageal pain. Aliment Pharmacol Ther. 2011 May;33(10):1113-22. doi: 10.1111/j.1365-2036.2011.04629.x. Epub 2011 Mar 16. PMID: 21410733.

3: Krarup AL, Ny L, Gunnarsson J, Hvid-Jensen F, Zetterstrand S, Simrén M, Funch-Jensen P, Hansen MB, Drewes AM. Randomized clinical trial: inhibition of the TRPV1 system in patients with nonerosive gastroesophageal reflux disease and a partial response to PPI treatment is not associated with analgesia to esophageal experimental pain. Scand J Gastroenterol. 2013 Mar;48(3):274-84. doi: 10.3109/00365521.2012.758769. Epub 2013 Jan 16. PMID: 23320520.

4: Miller F, Björnsson M, Svensson O, Karlsten R. Experiences with an adaptive design for a dose-finding study in patients with osteoarthritis. Contemp Clin Trials. 2014 Mar;37(2):189-99. doi: 10.1016/j.cct.2013.12.007. Epub 2014 Jan 3. PMID: 24394343.

5: Vela MF. Medical treatments of GERD: the old and new. Gastroenterol Clin North Am. 2014 Mar;43(1):121-33. doi: 10.1016/j.gtc.2013.12.001. Epub 2013 Dec 31. PMID: 24503363.

6: Garami A, Shimansky YP, Rumbus Z, Vizin RCL, Farkas N, Hegyi J, Szakacs Z, Solymar M, Csenkey A, Chiche DA, Kapil R, Kyle DJ, Van Horn WD, Hegyi P, Romanovsky AA. Hyperthermia induced by transient receptor potential vanilloid-1 (TRPV1) antagonists in human clinical trials: Insights from mathematical modeling and meta-analysis. Pharmacol Ther. 2020 Apr;208:107474. doi: 10.1016/j.pharmthera.2020.107474. Epub 2020 Jan 9. PMID: 31926897.

7: Kort ME, Kym PR. TRPV1 antagonists: clinical setbacks and prospects for future development. Prog Med Chem. 2012;51:57-70. doi: 10.1016/B978-0-12-396493-9.00002-9. PMID: 22520471.

8: Ängeby Möller K, Berge OG, Finn A, Stenfors C, Svensson CI. Using gait analysis to assess weight bearing in rats with Freund׳s complete adjuvant- induced monoarthritis to improve predictivity: Interfering with the cyclooxygenase and nerve growth factor pathways. Eur J Pharmacol. 2015 Jun 5;756:75-84. doi: 10.1016/j.ejphar.2015.02.050. Epub 2015 Mar 16. PMID: 25792342.

9: Parkinson J, Visser SA, Jarvis P, Pollard C, Valentin JP, Yates JW, Ewart L. Translational pharmacokinetic-pharmacodynamic modeling of QTc effects in dog and human. J Pharmacol Toxicol Methods. 2013 Nov-Dec;68(3):357-66. doi: 10.1016/j.vascn.2013.03.007. Epub 2013 Apr 6. PMID: 23567074.

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