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[MCE]: New Small Molecules for September 2021

[MCE]: New Small Molecules for September 2021

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 30,000 bioactive molecules in stock
• Target 500+ 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
• Data sheet with detailed biological information
• High purity & competitive prices
• Delivery within 24 hours

 

CAS No.: 315698-36-3
MLS1547
Research Area: Dopamine Receptor/ Neurological Disease

• Highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=1.2 μM ).
• Stimulates D2R G protein-mediated signaling (EC50=0.37 μM in a calcium mobilization assay) and acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R

Solubility: DMSO : 50 mg/mL (140.91 mM; Need ultrasonic)

 

CAS No.: 155428-00-5
Alniditan dihydrochloride
Research Area: 5-HT Receptor/Migraine

• Potent 5-HT1B and 5-HT1D receptors agonist with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and 5-HT1D receptors, respectively.
• Has migraine-preventive effects.

Solubility: DMSO : 62.5 mg/mL (166.52 mM; Need ultrasonic)

 

CAS No.: 1805789-54-1
Samuraciclib hydrochloride
Research Area: CDK7 Inhibitor/Breast Cancer

• Potent, selective, ATP-competitive and orally active CDK7 inhibitor (IC50=41 nM).
• Displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2, CDK5 and CDK9, respectively.
• Inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM and induces apoptosis.

Solubility: DMSO : 100 mg/mL (232.03 mM; Need ultrasonic)
H2O : 55 mg/mL (127.62 mM; Need ultrasonic)

 

CAS No.: 1929519-13-0
TAK-041
Research Area: GPR139/Schizophrenia

• Potent and selective GPR139 agonist with an EC50 of 22 nM.
• Has the potential for the research of negative symptoms associated with schizophrenia.

Solubility: DMSO : 100 mg/mL (254.89 mM; Need ultrasonic)

 

CAS No.: 169939-94-0
Ruboxistaurin
Research Area: PKC/Diabetic Peripheral Neuropathy

• Orally active, selective PKC beta (PKCβ) inhibitor (Ki=2 nM) and inhibits the PKC beta I (IC50=4.7 nM) and PKC beta II (IC50=5.9 nM) isozymes.
• Exhibits ATP dependent competitive inhibition of PKC beta I and is selective for PKC in comparison to other ATP dependent kinases (protein kinase A, calcium calmodulin, casein kinase, src tyrosine kinase).

Solubility: DMSO : 50 mg/mL (106.71 mM; ultrasonic and warming to 60°C)

 

CAS No.: 1414976-20-7
Vazegepant hydrochloride
Research Area: CGRP Receptor/Migraine/COVID-19

• High affinity antagonist of the CGRP receptor (hCGRP Ki=0.023 nM) and the first intranasal gepant for migraine.
• Has the potential for the research of the COVID-19 associated pulmonary inflammation.

Solubility: DMSO : 50 mg/mL (74.05 mM; Need ultrasonic)
H2O : 50 mg/mL (74.05 mM; Need ultrasonic)

 

Renilla-Firefly Luciferase Dual Assay Kit

MCE Renilla-Firefly Luciferase Dual Assay Kit contains high-purity D-Luciferin, coelenterazine and proprietary reaction buffer. This product is ideal for the detection of both Firefly luciferase and Renilla luciferase in mammalian cells.

 

Antibody-drug conjugate (ADC)

Antibody-drug conjugate (ADC), a chimeric or humanized monoclonal antibody tethered to a highly potent drug (payload) through a cleavable or non-cleavable linker, is an emerging novel class of anticancer drugs and has great potential to make a paradigm shift in cancer chemotherapy. The key factors to design antibody-drug conjugates are the rational selections of payload, linker or drug-linker conjugate, antibody, and conjugation strategy.
MCE can provide one-stop services for the design, synthesis, analysis, purification, optimization, detection and evaluation of 900+ ADC-related products (ADC Cytotoxin, ADC Linker, Drug-Linker Conjugates for ADC, and ADC).

Product Categories Service Categories Our Advantages
ADC Cytotoxin Custom synthesis Extensive product categories
ADC Linker Conjugation service Strong synthesis ability
Drug-linker Conjugate for ADC Purification service Innovation ability
Antibody-drug Conjugate (ADC) Analysis service Extensive cooperation

 

Recent Publications Citing Use of MCE Products

Nature. 2021 Aug;596(7871):
291-295..
Cell.2021 Jul
22;184(15):
4032-4047.e31.

Science.2021 Jul 30;
373(6554):547-555.
Immunity. 2021 Aug 10;54(8):
1728-1744.e7.

 

Cell Signaling Pathways