AM1241|cas 444912-48-5|DC Chemicals

Cas No.:	444912-48-5
Chemical Name:	(2-Iodo-5-nitrophenyl)(1-((1-methylpiperidin-2-yl)methyl)-1H-Indol-3-yl)methanone
Synonyms:	(2-Iodo-5-nitrophenyl)(1-((1-methylpiperidin-2-yl)methyl)-1H-Indol-3-yl)methanone;AM1241;(2-Iodo-5-nitrophenyl)[1-[(1-methyl-2-piperidinyl)methyl]-1H-indol-3-yl]methanone;(r,s)-am1241;AM-1241;(R,S)-3-(2-Iodo-5-nitrobenzoyl)-1-(1-methyl-2-piperidinylmethyl)-1H-indole
SMILES:	O=[N+]([O-])C1=CC(=C(I)C=C1)C(=O)C2C3C(=CC=CC=3)N(CC4N(C)CCCC4)C=2
Formula:	C₂₂H₂₂N₃O₃I
M.Wt:	503.33238
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	AM1241 is a potent, typical[2] and selective CB2 receptor agonist, with a Ki of 3.4 nM in a mouse spleen, and the Ki for CB1 receptor in rat brain is 280 nM, 82-fold selectivity for the CB2 receptor in rodent tissue[1]. AM1241 relieves migraine, stroke, and neuropathic pain，also has a potent effect on Parkinson's disease[2]. AM1241 prevents oxidative damage and activates STAT3 through the phosphorylation of Akt and Erk1/2[3].
Target:	Ki: 3.4 nM (Mouse spleen CB2 receptor), 280 nM (Rat brain CB1 receptor)[1]
In Vivo:	AM1241 (0.1-3 mg/kg, i.p.) dose-dependently inhibits sensory hypersensitivity in rats. AM1241 inhibits tactile hypersensitivity and thermal hypersensitivity at 1 mg/kg and 3 mg/kg, respectively, in mice lacking the CB1 receptor[1]. AM1241 (0.75, 1.5, 3, 6, 12 mg/kg, i.p.) alleviates MPTP-induced Parkinson's disease and promotes the regeneration of dopaminergic (DA) neurons in PD mice[2].
In Vitro:	AM1241 is a potent and selective CB2 receptor agonist, with a Ki of 3.4 nM in a mouse spleen, and the Ki for CB1 receptor in rat brain is 280 nM, 82-fold selectivity for the CB2 receptor in rodent tissue[1]. AM1241 decreases oxidative stress levels, enhances the production of paracrine growth factors, decreases TGF-β1 and PDGF levels, activates Stat3 via the phosphorylation of Akt and Erk1/2[3].
References:	[1]. Ibrahim MM, et al. Activation of CB2 cannabinoid receptors by AM1241 inhibits experimental neuropathic pain: pain inhibition by receptors not present in the CNS. Proc Natl Acad Sci U S A. 2003 Sep 2;100(18):10529-33. [2]. Shi J, et al. AM1241 alleviates MPTP-induced Parkinson's disease and promotes the regeneration of DA neurons in PD mice. Oncotarget. 2017 Jun 29;8(40):67837-67850. [3]. Han D, et al. Activation of cannabinoid receptor type II by AM1241 protects adipose-derived mesenchymal stem cells from oxidative damage and enhances their therapeutic efficacy in myocardial infarction mice via Stat3 activation. Oncotarget. 2017 May 4;8(39):64853-64866.

Cat. No.	Product name	Field of application
DC31074	Isopropyl myristate	Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC79609	NCGC00685960	NCGC00685960 is a Nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 < 10  nM. NCGC00685960 has potent antitumor activity. NCGC00685960 increases H3K27 trimethylation levels in ovarian cancer cells and inhibits α-SMA expression in NNMT-expressing ovarian fibroblasts. NCGC00685960 reduces 1-MNA levels, reverses SAM and H3K27 hypomethylation and significantly impairs collagen contractility in cancer-associated fibroblasts (CAFs). NCGC00685960 can be used for cancers research.
DC77831	Vicadrostat	Vicadrostat (compound 29 A) is a potent and selective inhibitor of aldosterone synthase(CYP11B2) with an IC50 of 16 nM. It exhibits potential in renal disease, diabetic nephropathy, cardiovascular diseases and fibrotic disorder research.
DC77813	Zeltociclib	Zeltociclib is a cyclin-dependent kinase inhibitor with antitumor effects.
DC77714	S3226	S3226 is an inhibitor for Na+/H+ exchange subtype 3 (NHE3) with an IC50 of 0.2 µmol/L in rat NHE3 transfected fibroblasts. S3226 exhibits protective activity in rat ischemia-induced acute renal failure models.
DC77387	AUR1545	AUR1545 is a selective degrader of KAT2A and KAT2B. AUR1545 can be used in the cancer research, including studies on AML (Acute myeloid leukemia), SCLC (Small-cell carcinoma), and NEPC (Neuroendocrine Prostate Cancer).
DC77822	JNJ-77242113 (Icotrokinr)	Icotrokinra (JNJ-77242113, JNJ-2113, PN-235) is an orally available and selective antagonist of the IL-23 receptor. It also inhibits IL-23–induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM and suppresses IL-23–induced IFN-γ production in NK cells with an IC50 of 18.4 pM. It also exhibits anti-inflammatory activity in a TNBS-induced colitis model in rats and holds potential for studying psoriasis, psoriatic arthritis, and inflammatory bowel disease.
DC77088	T025	T025 is as an orally available and potent inhibitor of Cdc2‐like kinases (CLKs) with an IC50s of 0.93 nM, 1 nM, 14 nM, 1.5 nM for CLK1, CLK2, CLK3, DYRK1B respectively. It exhibits anti‐tumor efficacy and can be used in MYC‐driven cancer research.
DC75868	AZ14133346	AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.
DC75865	TI17	TI17 represents a novel class of targeted anticancer agents that specifically disrupt DNA damage repair mechanisms in malignant cells.