LY2828360
featured

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

MedKoo CAT#: 527492

CAS#: 1231220-79-3

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


Chemical Structure

img
LY2828360
CAS# 1231220-79-3

Theoretical Analysis

MedKoo Cat#: 527492
Name: LY2828360
CAS#: 1231220-79-3
Chemical Formula: C22H27ClN6O
Exact Mass: 426.19
Molecular Weight: 426.949
Elemental Analysis: C, 61.89; H, 6.37; Cl, 8.30; N, 19.68; O, 3.75

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 weeks
100mg USD 750 2 weeks
200mg USD 1250 2 weeks
500mg USD 1850 2 weeks
1g USD 2950 2 weeks
2g USD 4650 2 weeks
Bulk inquiry

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:
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/

Solubility Data

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

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.

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. 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: 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.
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.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

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.