LY2828360 | CAS#1231220-79-3 | CB2 agonist

MedKoo Cat#: 527492 | Name: LY2828360

Description:

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

LY2828360 is a novel potent, selective, and efficacious CB2 agonist.

Chemical Structure

LY2828360

CAS#1231220-79-3

Theoretical Analysis

MedKoo Cat#: 527492

Name: LY2828360

CAS#: 1231220-79-3

Chemical Formula: C22H27ClN6O

Exact Mass: 426.1935

Molecular Weight: 426.95

Elemental Analysis: C, 61.89; H, 6.37; Cl, 8.30; N, 19.68; O, 3.75

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 weeks
100mg	USD 750.00	2 weeks
200mg	USD 1,250.00	2 weeks
500mg	USD 1,850.00	2 weeks
1g	USD 2,950.00	2 weeks
2g	USD 4,650.00	2 weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

LY 2828360; LY-2828360; LY2828360

IUPAC/Chemical Name

8-(2-Chloro-phenyl)-2-methyl-6-(4-methyl-piperazin-1-yl)-9-(tetrahydro-pyran-4-yl)-9H-purine

InChi Key

UCMNDPDJRSEZPL-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H27ClN6O/c1-15-24-21(28-11-9-27(2)10-12-28)19-22(25-15)29(16-7-13-30-14-8-16)20(26-19)17-5-3-4-6-18(17)23/h3-6,16H,7-14H2,1-2H3

SMILES Code

CN1CCN(C2=C3N=C(C4=CC=CC=C4Cl)N(C5CCOCC5)C3=NC(C)=N2)CC1

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:

LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist.

In vitro activity:

In vitro, LY2828360 was a slowly acting but efficacious G protein-biased CB2 agonist, inhibiting cAMP accumulation and activating extracellular signal-regulated kinase 1/2 signaling while failing to recruit arrestin, activate inositol phosphate signaling, or internalize CB2 receptors. Reference: Mol Pharmacol. 2018 Feb;93(2):49-62. https://pubmed.ncbi.nlm.nih.gov/29192123/

In vivo activity:

In ddC-treated CB2f/f mice, LY2828360 suppressed development of morphine tolerance and reversed established morphine tolerance, albeit with greater efficacy in male compared to female mice. Reference: Pharmacol Res. 2023 Jan;187:106560. https://pubmed.ncbi.nlm.nih.gov/36417942/

	Solvent	mg/mL	mM
Solubility
	Chloroform	30.0	70.27
	DMSO	20.8	48.79

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 426.95 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. Ao Z, Cai H, Wu Z, Song S, Karahan H, Kim B, Lu HC, Kim J, Mackie K, Guo F. Tubular human brain organoids to model microglia-mediated neuroinflammation. Lab Chip. 2021 Jul 13;21(14):2751-2762. doi: 10.1039/d1lc00030f. PMID: 34021557; PMCID: PMC8493632. 2. Lin X, Dhopeshwarkar AS, Huibregtse M, Mackie K, Hohmann AG. Slowly Signaling G Protein-Biased CB2 Cannabinoid Receptor Agonist LY2828360 Suppresses Neuropathic Pain with Sustained Efficacy and Attenuates Morphine Tolerance and Dependence. Mol Pharmacol. 2018 Feb;93(2):49-62. doi: 10.1124/mol.117.109355. Epub 2017 Nov 30. PMID: 29192123; PMCID: PMC5749492. 1. Ao Z, Cai H, Wu Z, Song S, Karahan H, Kim B, Lu HC, Kim J, Mackie K, Guo F. Tubular human brain organoids to model microglia-mediated neuroinflammation. Lab Chip. 2021 Jul 13;21(14):2751-2762. doi: 10.1039/d1lc00030f. PMID: 34021557; PMCID: PMC8493632. 2. Lin X, Dhopeshwarkar AS, Huibregtse M, Mackie K, Hohmann AG. Slowly Signaling G Protein-Biased CB2 Cannabinoid Receptor Agonist LY2828360 Suppresses Neuropathic Pain with Sustained Efficacy and Attenuates Morphine Tolerance and Dependence. Mol Pharmacol. 2018 Feb;93(2):49-62. doi: 10.1124/mol.117.109355. Epub 2017 Nov 30. PMID: 29192123; PMCID: PMC5749492. 3. Carey LM, Xu Z, Rajic G, Makriyannis A, Romero J, Hillard C, Mackie K, Hohmann AG. Peripheral sensory neuron CB2 cannabinoid receptors are necessary for both CB2-mediated antinociceptive efficacy and sparing of morphine tolerance in a mouse model of anti-retroviral toxic neuropathy. Pharmacol Res. 2023 Jan;187:106560. doi: 10.1016/j.phrs.2022.106560. Epub 2022 Nov 20. PMID: 36417942; PMCID: PMC9845180. 4. Iyer V, Slivicki RA, Thomaz AC, Crystal JD, Mackie K, Hohmann AG. The cannabinoid CB2 receptor agonist LY2828360 synergizes with morphine to suppress neuropathic nociception and attenuates morphine reward and physical dependence. Eur J Pharmacol. 2020 Nov 5;886:173544. doi: 10.1016/j.ejphar.2020.173544. Epub 2020 Sep 5. PMID: 32896549; PMCID: PMC7694697.

In vitro protocol:

In vivo protocol:

1. Carey LM, Xu Z, Rajic G, Makriyannis A, Romero J, Hillard C, Mackie K, Hohmann AG. Peripheral sensory neuron CB2 cannabinoid receptors are necessary for both CB2-mediated antinociceptive efficacy and sparing of morphine tolerance in a mouse model of anti-retroviral toxic neuropathy. Pharmacol Res. 2023 Jan;187:106560. doi: 10.1016/j.phrs.2022.106560. Epub 2022 Nov 20. PMID: 36417942; PMCID: PMC9845180. 2. Iyer V, Slivicki RA, Thomaz AC, Crystal JD, Mackie K, Hohmann AG. The cannabinoid CB2 receptor agonist LY2828360 synergizes with morphine to suppress neuropathic nociception and attenuates morphine reward and physical dependence. Eur J Pharmacol. 2020 Nov 5;886:173544. doi: 10.1016/j.ejphar.2020.173544. Epub 2020 Sep 5. PMID: 32896549; PMCID: PMC7694697.

1: Lin X, Dhopeshwarkar AS, Huibregtse M, Mackie K, Hohmann AG. Slowly Signaling G Protein-Biased CB(2) Cannabinoid Receptor Agonist LY2828360 Suppresses Neuropathic Pain with Sustained Efficacy and Attenuates Morphine Tolerance and Dependence. Mol Pharmacol. 2018 Feb;93(2):49-62. doi: 10.1124/mol.117.109355. Epub 2017 Nov 30. PubMed PMID: 29192123.