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MedKoo Cat#: 524207 | Name: AMG-009
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Description:

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

AMG 009 is an orally active, small molecule CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) and DP (D prostanoid) dual antagonist, which was in preclinical development in the US for the treatment of asthma and allergic rhinitis.

Chemical Structure

AMG-009
AMG-009
CAS#1027847-67-1

Theoretical Analysis

MedKoo Cat#: 524207

Name: AMG-009

CAS#: 1027847-67-1

Chemical Formula: C26H26Cl2N2O7S

Exact Mass: 580.0838

Molecular Weight: 581.46

Elemental Analysis: C, 53.71; H, 4.51; Cl, 12.19; N, 4.82; O, 19.26; S, 5.51

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,350.00 Ready to ship
500mg USD 2,950.00 Ready to ship
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Related CAS #
No Data
Synonym
AMG-009; AMG 009; AMG009.
IUPAC/Chemical Name
2-(4-(4-(butylcarbamoyl)-2-((2,4-dichlorophenyl)sulfonamido)phenoxy)-3-methoxyphenyl)acetic acid
InChi Key
DKSKRBVXRDGYAS-UHFFFAOYSA-N
InChi Code
InChI=1S/C26H26Cl2N2O7S/c1-3-4-11-29-26(33)17-6-9-21(37-22-8-5-16(13-25(31)32)12-23(22)36-2)20(14-17)30-38(34,35)24-10-7-18(27)15-19(24)28/h5-10,12,14-15,30H,3-4,11,13H2,1-2H3,(H,29,33)(H,31,32)
SMILES Code
CCCCNC(=O)c1ccc(c(c1)NS(=O)(=O)c2ccc(cc2Cl)Cl)Oc3ccc(cc3OC)CC(=O)O
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, not in water
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
Biological target:
AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 581.46 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.

Recalculate based on batch purity %
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
1: Bi M, Kyad A, Kiang YH, Alvarez-Nunez F, Alvarez F. Enhancing and sustaining AMG 009 dissolution from a matrix tablet via microenvironmental pH modulation and supersaturation. AAPS PharmSciTech. 2011 Dec;12(4):1157-62. doi: 10.1208/s12249-011-9679-x. Epub 2011 Sep 13. Erratum in: AAPS PharmSciTech. 2011 Dec;12(4):1466. Kiang, Yuan-Hon [corrected to Kiang, Y-H]. PMID: 21913050; PMCID: PMC3225532. 2: Bi M, Kyad A, Alvarez-Nunez F, Alvarez F. Enhancing and sustaining AMG 009 dissolution from a bilayer oral solid dosage form via microenvironmental pH modulation and supersaturation. AAPS PharmSciTech. 2011 Dec;12(4):1401-6. doi: 10.1208/s12249-011-9710-2. Epub 2011 Oct 20. PMID: 22012200; PMCID: PMC3225540. 3: Liu J, Li AR, Wang Y, Johnson MG, Su Y, Shen W, Wang X, Lively S, Brown M, Lai S, Gonzalez Lopez De Turiso F, Xu Q, Van Lengerich B, Schmitt M, Fu Z, Sun Y, Lawlis S, Seitz L, Danao J, Wait J, Ye Q, Tang HL, Grillo M, Collins TL, Sullivan TJ, Medina JC. Discovery of AMG 853, a CRTH2 and DP Dual Antagonist. ACS Med Chem Lett. 2011 Mar 2;2(5):326-30. doi: 10.1021/ml1002234. PMID: 24900313; PMCID: PMC4018074. 4: Liu J, Fu Z, Wang Y, Schmitt M, Huang A, Marshall D, Tonn G, Seitz L, Sullivan T, Lucy Tang H, Collins T, Medina J. Discovery and optimization of CRTH2 and DP dual antagonists. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6419-23. doi: 10.1016/j.bmcl.2009.09.052. Epub 2009 Sep 17. PMID: 19804971. 5: Wang Y, Fu Z, Schmitt M, Wang X, Shen W, Rickel E, Martin T, Budelsky A, Marshall D, Collins T, Tang HL, Medina JC, Liu JJ. Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism. Bioorg Med Chem Lett. 2012 Jan 1;22(1):367-70. doi: 10.1016/j.bmcl.2011.10.123. Epub 2011 Nov 9. PMID: 22119474. 6: Liu JJ, Wang Y, Johnson MG, Li AR, Shen W, Wang X, Su Y, Brown M, Van Lengerich B, Rickel E, Martin T, Budelsky A, Seitz L, Danao J, Tang HL, Collins T, Medina JC. Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1686-9. doi: 10.1016/j.bmcl.2011.12.107. Epub 2011 Dec 30. PMID: 22264478. 7: Morgan RE, van Staden CJ, Chen Y, Kalyanaraman N, Kalanzi J, Dunn RT 2nd, Afshari CA, Hamadeh HK. A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov;136(1):216-41. doi: 10.1093/toxsci/kft176. Epub 2013 Aug 16. PMID: 23956101. 8: Johnson MG, Liu JJ, Li AR, van Lengerich B, Wang S, Medina JC, Collins TL, Danao J, Seitz L, Willee A, D'Souza W, Budelsky AL, Fan PW, Wong SG. Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP. Bioorg Med Chem Lett. 2014 Jul 1;24(13):2877-80. doi: 10.1016/j.bmcl.2014.04.092. Epub 2014 May 4. PMID: 24825301. 9: Nautiyal M, Qasem RJ, Fallon JK, Wolf KK, Liu J, Dixon D, Smith PC, Mosedale M. Characterization of primary mouse hepatocyte spheroids as a model system to support investigations of drug-induced liver injury. Toxicol In Vitro. 2021 Feb;70:105010. doi: 10.1016/j.tiv.2020.105010. Epub 2020 Oct 3. PMID: 33022361; PMCID: PMC7736539. 10: Ryan J, Morgan RE, Chen Y, Volak LP, Dunn RT 2nd, Dunn KW. Intravital Multiphoton Microscopy with Fluorescent Bile Salts in Rats as an In Vivo Biomarker for Hepatobiliary Transport Inhibition. Drug Metab Dispos. 2018 May;46(5):704-718. doi: 10.1124/dmd.117.079277. Epub 2018 Feb 21. PMID: 29467212. 11: Bi M, Alvarez-Nunez F, Alvarez F. Evaluating and modifying Johanson's rolling model to improve its predictability. J Pharm Sci. 2014 Jul;103(7):2062-2071. doi: 10.1002/jps.24012. Epub 2014 May 19. PMID: 24840775.

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CT-2584

CT-2584