Home > Products > Novel inhibitors

MIPS-521

  Cat. No.:  DC57090   Featured
Chemical Structure
1146188-19-3
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
MIPS521 is a positive allosteric modulator of the adenosine A1 receptor.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1146188-19-3
Chemical Name: MIPS-521
Synonyms: MIPS-521;MIPS 521;MIPS521
SMILES: O=C(C1=C(N)SC=C1C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)C3=CC=C(Cl)C=C3
Formula: C19H10ClF6NOs
M.Wt: 449.795
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95). MIPS521 exhibits pain-relieving effects in vivo[1][2].
Target: A1AR
In Vivo: MIPS521 (1-30 μg in 10 μL; intrathecal administration) reverses mechanical hyperalgesia in rats, promoting robust antinociception[2]. MIPS521 (10 μg in 10 μL; intrathecal administration) significantly reduces spontaneous pain in a conditioned place preference model[2]. MIPS521 (1-30 μg in 10 μL; intrathecal administration) reduces eEPSCs in spinal cord from nerve-injured rats, with a pEC50 of 6.9. The maximum MIPS521-induced decrease in synaptic current amplitude is significantly greater in nerve-injured rats than in sham surgery controls[2]. Animal Model: Male and female Sprague-Dawley rats (7-12 weeks) were performed a partial nerve ligation (PNL) or sham surgery[2] Dosage: 1, 3, 10, 30 μg in 10 μL Administration: Intrathecal administration Result: Reduced eEPSCs in spinal cord from nerve-injured rats and reversed mechanical hyperalgesia.
In Vitro: MIPS521 (compound 13o) (3-10 μM) improves the ability of R-PIA to promote A1AR-mediated ERK1/2 phosphorylation[1]. MIPS521 (0.3-30 μM; pretreament for 10 min, co-treatment for 30 min) produces a concentration-dependent potentiation of signalling by ADO in an inhibition of cAMP assay (expressed as a percentage of the inhibition of 3 μM forskolin-mediated cAMP) in CHO cells[2].
References: [1]. Aurelio L, et, al. Allosteric modulators of the adenosine A1 receptor: synthesis and pharmacological evaluation of 4-substituted 2-amino-3-benzoylthiophenes. J Med Chem. 2009 Jul 23;52(14):4543-7. [2]. Draper-Joyce CJ, et, al. Positive allosteric mechanisms of adenosine A 1 receptor-mediated analgesia. Nature. 2021 Sep;597(7877):571-576.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC60781 TRPC6 activator compound 2 TRPC6 activator compound 2 is selective activator of TRPC6 that does not potentiate TRPC3 and mTRPC7. Comp2 is able to cross BBB.
DC66546 R-Sirpiglenastat R-Sirpiglenastat is the R- isomer of Sirpiglenastat(DRP-104).Sirpiglenastat (DRP104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.
DC60597 AZD0780 AZD0780 is the first oral small molecule PCSK9 inhibitor for the treatment of hypercholesterolemia.
DC90056 PLX-5622 HCl form (water solubility form) PLX5622 is the HCl salt form of PLX-5622, which has better water solubility.PLX-5622 is a highly selective brain-penetrant CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM) allowing for extended and specific microglial elimination, preceding and during pathology development.
DC60559 PT-179 PT-179 is a new orthogonal immunomodulatory drug (IMiD) derivative that binds CRBN but does not induce degradation of off-target proteins. PT-179 potently degrades proteins fused to SD40 at either the N or C terminus.
DC65830 1-M-PES(1-Methoxy-5-methylphenazinium ethyl sulfate) 1-m-PES is an electron mediator which has higher stability of solutions than 1-Methoxy PMS. The stability in neutral to alkali conditions has been extremely improved with 1-Methoxy PES. 1-M-PES is a stable small-molecular compound and it has an equal or higher thermal stability than diaphorase. The 1-Methoxy PES solution can be stored long term.
DC65821 Upadacitinib hemihydrate Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.
DC65697 HDAC6 inhibitor 4510 A novel and seletive HDAC6 inhibitor.
DC65676 Fenretinide Glucuronide Monosodium Salt Fenretinide Glucuronide Monosodium Salt, is the metabolite of Fenretinide (F250000), which is a synthetic retinoid deriverative, substances related to vitamin A. They are also shown to be used for the treatment of cancer, as well as in the treatment of cystic fibrosis, rheumatoid arthritis, acne, and psoriasis.
DC60500 NVS-STG2 NVS-STG2 is a molecular glue that targets STING and activates STING-mediated immune signaling. NVS-STG2 induces higher-order oligomerization of human STING by binding to pockets between adjacent STING dimer transmembrane domains, effectively acting as a molecular glue. NVS-STGI enhances the activity of cGAMP by inducing the formation of more abundant and larger oligomers. NVS-STG2 produces antitumor activity in animal models.
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia