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MedKoo Cat#: 562549 | Name: DREADD agonist 21
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Description:

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

DREADD agonist 21 is a muscarinic hM3Dq DREADD receptor agonist.

Chemical Structure

DREADD agonist 21
DREADD agonist 21
CAS#56296-18-5

Theoretical Analysis

MedKoo Cat#: 562549

Name: DREADD agonist 21

CAS#: 56296-18-5

Chemical Formula: C17H18N4

Exact Mass: 278.1531

Molecular Weight: 278.36

Elemental Analysis: C, 73.35; H, 6.52; N, 20.13

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
10mg USD 585.00 2 Weeks
25mg USD 950.00 2 Weeks
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Related CAS #
No Data
Synonym
DREADD agonist 21; DREADD-agonist-21; DREADD agonist-21;
IUPAC/Chemical Name
11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
InChi Key
JCBYXNSOLUVGTF-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H18N4/c1-2-6-14-13(5-1)17(21-11-9-18-10-12-21)20-16-8-4-3-7-15(16)19-14/h1-8,18-19H,9-12H2
SMILES Code
C12=CC=CC=C1NC3=CC=CC=C3C(N4CCNCC4)=N2
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
View handling instruction
Biological target:
DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).
In vitro activity:
This study has previously reported that both C21 and perlapine potently activated hM3Dq in Chinese hamster ovary (CHO) cells transfected cells in vitro,30 and their data are confirmed here with C21 and perlapine stimulating calcium mobilization at hM3Dq with a pEC50 of 8.48 ± 0.05 and 8.08 ± 0.05, respectively (Figure S1). Reference: ACS Pharmacol Transl Sci. 2018 Sep 14;1(1):61-72. https://pubmed.ncbi.nlm.nih.gov/30868140/
In vivo activity:
The brain-gut-microbiota axis has a crucial role in bidirectional interactions between the brain and the gastrointestinal microbiota. This study investigated whether repeated administration of CNO or C21 could influence the gut microbiota and short-chain fatty acids (SCFAs) in feces of adult mice. The data suggest that repeated administration of CNO or C21 contributes to an unusual organization of the gut microbiota in adult mice. Reference: Brain Res Bull. 2021 Aug;173:66-73. https://pubmed.ncbi.nlm.nih.gov/34004259/
Solvent mg/mL mM
Solubility
DMSO:PBS (pH 7.2) (1:1) 0.5 1.80
Ethanol 29.6 106.39
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 278.36 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
Formulation protocol:
1. Thompson KJ, Khajehali E, Bradley SJ, Navarrete JS, Huang XP, Slocum S, Jin J, Liu J, Xiong Y, Olsen RHJ, Diberto JF, Boyt KM, Pina MM, Pati D, Molloy C, Bundgaard C, Sexton PM, Kash TL, Krashes MJ, Christopoulos A, Roth BL, Tobin AB. DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo. ACS Pharmacol Transl Sci. 2018 Sep 14;1(1):61-72. doi: 10.1021/acsptsci.8b00012. Epub 2018 Jul 27. PMID: 30868140; PMCID: PMC6407913. 2. Guo W, Wan X, Ma L, Zhang J, Hashimoto K. Abnormalities in the composition of the gut microbiota in mice after repeated administration of DREADD ligands. Brain Res Bull. 2021 Aug;173:66-73. doi: 10.1016/j.brainresbull.2021.05.012. Epub 2021 May 15. PMID: 34004259. 3. Roselli V, Guo C, Huang D, Wen D, Zona D, Liang T, Ma YY. Prenatal alcohol exposure reduces posterior dorsomedial striatum excitability and motivation in a sex- and age-dependent fashion. Neuropharmacology. 2020 Dec 1;180:108310. doi: 10.1016/j.neuropharm.2020.108310. Epub 2020 Sep 17. PMID: 32950559; PMCID: PMC7773417.
In vitro protocol:
1. Thompson KJ, Khajehali E, Bradley SJ, Navarrete JS, Huang XP, Slocum S, Jin J, Liu J, Xiong Y, Olsen RHJ, Diberto JF, Boyt KM, Pina MM, Pati D, Molloy C, Bundgaard C, Sexton PM, Kash TL, Krashes MJ, Christopoulos A, Roth BL, Tobin AB. DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo. ACS Pharmacol Transl Sci. 2018 Sep 14;1(1):61-72. doi: 10.1021/acsptsci.8b00012. Epub 2018 Jul 27. PMID: 30868140; PMCID: PMC6407913.
In vivo protocol:
1. Guo W, Wan X, Ma L, Zhang J, Hashimoto K. Abnormalities in the composition of the gut microbiota in mice after repeated administration of DREADD ligands. Brain Res Bull. 2021 Aug;173:66-73. doi: 10.1016/j.brainresbull.2021.05.012. Epub 2021 May 15. PMID: 34004259. 2. Roselli V, Guo C, Huang D, Wen D, Zona D, Liang T, Ma YY. Prenatal alcohol exposure reduces posterior dorsomedial striatum excitability and motivation in a sex- and age-dependent fashion. Neuropharmacology. 2020 Dec 1;180:108310. doi: 10.1016/j.neuropharm.2020.108310. Epub 2020 Sep 17. PMID: 32950559; PMCID: PMC7773417.
1: Giorgi A, Migliarini S, Galbusera A, Maddaloni G, Mereu M, Margiani G, Gritti M, Landi S, Trovato F, Bertozzi SM, Armirotti A, Ratto GM, De Luca MA, Tonini R, Gozzi A, Pasqualetti M. Brain-wide Mapping of Endogenous Serotonergic Transmission via Chemogenetic fMRI. Cell Rep. 2017 Oct 24;21(4):910-918. doi: 10.1016/j.celrep.2017.09.087. PubMed PMID: 29069598. 2: Sun JJ, Ray RS. Tg(Th-Cre)FI172Gsat (Th-Cre) defines neurons that are required for full hypercapnic and hypoxic reflexes. Biol Open. 2017 Aug 15;6(8):1200-1208. doi: 10.1242/bio.026823. PubMed PMID: 28684394; PubMed Central PMCID: PMC5576086. 3: Sun HX, Wang DR, Ye CB, Hu ZZ, Wang CY, Huang ZL, Yang SR. Activation of the ventral tegmental area increased wakefulness in mice. Sleep Biol Rhythms. 2017;15(2):107-115. doi: 10.1007/s41105-017-0094-x. Epub 2017 Feb 24. PubMed PMID: 28386207; PubMed Central PMCID: PMC5362655.