CT-1812 free base | CAS#1802632-22-9 | sigma-2/PGRMC1 antagonist

MedKoo Cat#: 555469 | Name: CT-1812 free base

Description:

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

CT-1812 is a first-in-class, orally available sigma-2/PGRMC1 antagonist (alpha beta oligomer receptor antagonist), is being developed by Cognition. sCT-1812 is a novel therapeutic candidate for Alzheimer's disease.

Chemical Structure

CT-1812 free base

CAS#1802632-22-9 (free base)

Theoretical Analysis

MedKoo Cat#: 555469

Name: CT-1812 free base

CAS#: 1802632-22-9 (free base)

Chemical Formula: C24H33NO4S

Exact Mass: 431.2130

Molecular Weight: 431.59

Elemental Analysis: C, 66.79; H, 7.71; N, 3.25; O, 14.83; S, 7.43

Price and Availability

Size	Price	Availability
100mg	USD 1,450.00	2 Weeks
200mg	USD 1,950.00	2 Weeks
500mg	USD 2,950.00	2 Weeks
1g	USD 4,850.00	2 Weeks

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Related CAS #

1802632-22-9 (free base) 2315504-28-8 (fumarate)

Synonym

CT-1812; CT 1812; CT1812; CT-1812 free base;

IUPAC/Chemical Name

2-(tert-butoxy)-4-(3-methyl-3-(5-(methylsulfonyl)isoindolin-2-yl)butyl)phenol

InChi Key

ISQAPFMBJFZOLG-UHFFFAOYSA-N

InChi Code

InChI=1S/C24H33NO4S/c1-23(2,3)29-22-13-17(7-10-21(22)26)11-12-24(4,5)25-15-18-8-9-20(30(6,27)28)14-19(18)16-25/h7-10,13-14,26H,11-12,15-16H2,1-6H3

SMILES Code

OC1=CC=C(CCC(C)(N2CC3=C(C=C(S(=O)(C)=O)C=C3)C2)C)C=C1OC(C)(C)C

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

>3 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

View handling instruction

Biological target:

Sigma-2 receptor antagonist 1 is a sigma-2 (σ-2) receptor antagonist.

In vitro activity:

CT1812 significantly increased CSF concentrations of Aβ oligomers in AD patient CSF, reduced concentrations of synaptic proteins and phosphorylated tau fragments, and reversed expression of many AD-related proteins dysregulated in CSF. Reference: Alzheimers Dement. 2021 Feb 8:10.1002/alz.12302. https://pubmed.ncbi.nlm.nih.gov/33559354/

In vivo activity:

CT1812 significantly and dose-dependently displaced Aβ oligomers bound to synaptic receptors in three independent preclinical models of AD, facilitated oligomer clearance into the CSF, increased synaptic number and protein expression in neurons, and improved cognitive performance in transgenic mice. Reference: Alzheimers Dement. 2021 Feb 8:10.1002/alz.12302. https://pubmed.ncbi.nlm.nih.gov/33559354/

	Solvent	mg/mL	mM
Solubility
	DMSO	250.0	579.25

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 431.59 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. Izzo NJ, Yuede CM, LaBarbera KM, Limegrover CS, Rehak C, Yurko R, Waybright L, Look G, Rishton G, Safferstein H, Hamby ME, Williams C, Sadlek K, Edwards HM, Davis CS, Grundman M, Schneider LS, DeKosky ST, Chelsky D, Pike I, Henstridge C, Blennow K, Zetterberg H, LeVine H 3rd, Spires-Jones TL, Cirrito JR, Catalano SM. Preclinical and clinical biomarker studies of CT1812: A novel approach to Alzheimer's disease modification. Alzheimers Dement. 2021 Feb 8:10.1002/alz.12302. doi: 10.1002/alz.12302. Epub ahead of print. PMID: 33559354; PMCID: PMC8349378.

In vitro protocol:

In vivo protocol:

1: Grundman M, Morgan R, Lickliter JD, Schneider LS, DeKosky S, Izzo NJ, Guttendorf R, Higgin M, Pribyl J, Mozzoni K, Safferstein H, Catalano SM. A phase 1 clinical trial of the sigma-2 receptor complex allosteric antagonist CT1812, a novel therapeutic candidate for Alzheimer's disease. Alzheimers Dement (N Y). 2019 Jan 23;5:20-26. doi: 10.1016/j.trci.2018.11.001. eCollection 2019. PubMed PMID: 30723776; PubMed Central PMCID: PMC6352291.