Org 27569 - ≥98%, high purity , CAS No.868273-06-7, Allosteric modulator of CB 1 receptor

Item Number
O129837
Grouped product items
SKUSizeAvailabilityPrice Qty
O129837-10mg
10mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$98.90
O129837-50mg
50mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$355.90

Potent CB 1 receptor allosteric modulator

Basic Description

Synonyms9GL | HMS3651O11 | EN300-60161 | 5-Chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide | AC-32888 | AS-56123 | Org27569 | ORG-27569 | 7YW2S3Z2CB | 6-(Trifluoromethyl)-1,4-benzothiadiazine-7-sulfonamide 1,1-dioxide | 5-chloro-3-ethyl-N-[
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsOrg 27569 is a CB1 receptor allosteric modulator. Exhibits increased binding of the CB1 agonist. Inhibits CB1 receptor antagonist effectiveness in vitro.Potent CB 1 receptor allosteric modulator (pEC 50 = 8.24). Significantly increases binding of the CB 1
Storage TempStore at 2-8°C
Shipped InWet ice
GradeMoligand™
Action TypeALLOSTERIC MODULATOR
Mechanism of actionAllosteric modulator of CB 1 receptor
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity.
A CB1 receptor allosteric modulator.

Associated Targets(Human)

CNR1 Tclin Cannabinoid receptor 1 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CNR1 Tclin Cannabinoid CB1 receptor (20913 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CNR2 Tchem Cannabinoid CB2 receptor (16942 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ARSA Tbio Cerebroside-sulfatase (655 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
POLK Tbio DNA polymerase kappa (8653 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EHMT2 Tchem Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (93046 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CBX1 Tbio Chromobox protein homolog 1 (92434 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RGS4 Tchem Regulator of G-protein signaling 4 (13867 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
pfk 6-phospho-1-fructokinase (7870 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 5-chloro-3-ethyl-N-[2-(4-piperidin-1-ylphenyl)ethyl]-1H-indole-2-carboxamide
INCHI InChI=1S/C24H28ClN3O/c1-2-20-21-16-18(25)8-11-22(21)27-23(20)24(29)26-13-12-17-6-9-19(10-7-17)28-14-4-3-5-15-28/h6-11,16,27H,2-5,12-15H2,1H3,(H,26,29)
InChi Key AHFZDNYNXFMRFQ-UHFFFAOYSA-N
Canonical SMILES CCC1=C(NC2=C1C=C(C=C2)Cl)C(=O)NCCC3=CC=C(C=C3)N4CCCCC4
Isomeric SMILES CCC1=C(NC2=C1C=C(C=C2)Cl)C(=O)NCCC3=CC=C(C=C3)N4CCCCC4
PubChem CID 44828492
Molecular Weight 409.95

Certificates

Certificate of Analysis(COA)

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Lot NumberCertificate TypeDateItem
F1525078Certificate of AnalysisJan 24, 2023 O129837

Chemical and Physical Properties

SolubilitySoluble to 100 mM in DMSO
SensitivityMoisture sensitive

Related Documents

References

1. Price MR, Baillie GL, Thomas A, Stevenson LA, Easson M, Goodwin R, McLean A, McIntosh L, Goodwin G, Walker G et al..  (2005)  Allosteric modulation of the cannabinoid CB1 receptor..  Mol Pharmacol,  68  (5): (1484-95).  [PMID:16113085] [10.1021/op500134e]
2. Fay JF, Farrens DL.  (2012)  A key agonist-induced conformational change in the cannabinoid receptor CB1 is blocked by the allosteric ligand Org 27569..  J Biol Chem,  287  (40): (33873-82).  [PMID:22846992] [10.1021/op500134e]

Solution Calculators