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

MedKoo CAT#: 522493

CAS#: 1093135-60-4 (free base)

Description: CPG-52364 a small molecule TLR7/8/9 antagonist, has recently completed phase 1 clinical trial for SLE therapy. Toll-like receptors (TLRs) are a family of type I transmembrane receptors and the central components of the innate immune system. Human TLR3, TLR7, TLR8, and TLR9 are expressed on endosomal membranes in the cells and recognize pathogenderived nucleic acid molecular patterns.5 However, recognition of endogenous immune complexes containing self-nucleic acids as PAMPs or DAMPs contributes to certain autoimmune diseases, such as systemic lupus erythematosus (SLE), psoriasis,7 arthritis, and multiple sclerosis.8 Therefore, inhibition of these recognition signals is expected to have therapeutic value.

Chemical Structure

CAS# 1093135-60-4 (free base)

Theoretical Analysis

MedKoo Cat#: 522493
Name: CPG-52364
CAS#: 1093135-60-4 (free base)
Chemical Formula: C27H36N6O3
Exact Mass: 492.28489
Molecular Weight: 492.624
Elemental Analysis: C, 65.83; H, 7.37; N, 17.06; O, 9.74

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Related CAS #: 1093135-60-4 (free base)   1093135-62-6 (sulfate)    

Synonym: CPG-52364; CPG 52364; CPG52364.

IUPAC/Chemical Name: 6,7-dimethoxy-2-(4-(4-methylpiperazin-1-yl)phenyl)-N-(2-morpholinoethyl)quinazolin-4-amine


InChi Code: InChI=1S/C27H36N6O3/c1-31-10-12-33(13-11-31)21-6-4-20(5-7-21)26-29-23-19-25(35-3)24(34-2)18-22(23)27(30-26)28-8-9-32-14-16-36-17-15-32/h4-7,18-19H,8-17H2,1-3H3,(H,28,29,30)


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

Preparing Stock Solutions

The following data is based on the product molecular weight 492.624 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

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1: Watanabe M, Kasai M, Tomizawa H, Aoki M, Eiho K, Isobe Y, Asano S. Dihydropyrrolo[2,3-d]pyrimidines: Selective Toll-Like Receptor 9 Antagonists from Scaffold Morphing Efforts. ACS Med Chem Lett. 2014 Oct 2;5(11):1235-9. doi: 10.1021/ml5003184. eCollection 2014 Nov 13. PubMed PMID: 25408837; PubMed Central PMCID: PMC4233361.

2: Thanou A, Merrill JT. Treatment of systemic lupus erythematosus: new therapeutic avenues and blind alleys. Nat Rev Rheumatol. 2014 Jan;10(1):23-34.
doi: 10.1038/nrrheum.2013.145. Epub 2013 Oct 8. Review. PubMed PMID: 24100460.

Additional Information

Related CAS#
1093135-60-4 ( CPG-52364 free base);
1093135-62-6 ( CPG-52364 sulfate)