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128381 Singapore.

 

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New Small Molecules from MCE for July 2020

New Small Molecules from MCE for July 2020

MedChemExpress (MCE) offers a wide range of high quality research chemicals and biochemicals including novel bioactive compounds, dye reagents, peptides and natural compounds for laboratory and scientific use.

• Over 25,000 bioactive molecules in stock
• Target 375 key proteins in 20+ signaling pathways
• Quality reports (LC/MS, NMR and HPLC) for each product
• Release more than 500 of the newest biochemicals per month
• High purity & competitive prices
• Data sheet with detailed biological information
• Delivery within 24 hours
• TRP Channel Agonist
MDR-652                                                   CAS No. : 1933528-96-1

MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity

Compound Screening Libraries

 

 

50 specific libraries for high throughput screening (HTS) and high content screening (HCS). Optimized for drug screening and new indication research.

• Dopamine Receptor Agonist
ML417                                   CAS No. : 1386162-69-1

ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.

Cell Signaling Pathway

• 5-HT Receptor Antagonist
SB-200646A                          CAS No. : 143797-62-0

SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.

• Recent Publication Citing used MCE

1. Nature. 2020 Jun;582(7813):561-565.
2. Nature. 2020 Jun 3. doi: 10.1038/s41586-020-2374-x.
3. Cell. 2020 May 28;181(5):1062-1079.e30.

• Histone Methyltransferase Inhibitor
AMI-1               CAS No. : 20324-87-2

AMI-1 is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 exerts PRMTs inhibitory effects by blocking peptide-substrate binding.

• HSP Inhibitor
HM03          CAS No. : 500565-15-1

HM03 is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 has anticancer activity.

 

Other New Products This Month

Setmelanotide (Melanocortin Receptor) Fluorometholone (Glucocorticoid Receptor) Didesmethylrocaglamide (Eukaryotic Initiation Factor (eIF))
Etanercept (TNF Receptor) Piromelatine (Melatonin Receptor) Saralasin TFA (Angiotensin Receptor)
Atosiban (Oxytocin Receptor) Terlipressin (Vasopressin Receptor) Cyclopentolate hydrochloride (mAChR)
Nadolol (Adrenergic Receptor) …