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Chemical Structure| 223499-30-7 Chemical Structure| 223499-30-7

Structure of YM-58483
CAS No.: 223499-30-7

Chemical Structure| 223499-30-7

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CAS No.: 223499-30-7

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YM-58483 is a selective calcium release-activated calcium channel (CRAC) inhibitor with high affinity for Orai1, with an IC50 value of 10 nM. YM-58483 has immunoregulatory and anti-inflammatory effects and can be used in research on autoimmune diseases and inflammation-related conditions.

Synonyms: BTP2

4.5 *For Research Use Only !

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Product Details of YM-58483

CAS No. :223499-30-7
Formula : C15H9F6N5OS
M.W : 421.32
SMILES Code : O=C(C1=C(C)N=NS1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2
Synonyms :
BTP2
MDL No. :MFCD00220976
InChI Key :XPRZIORDEVHURQ-UHFFFAOYSA-N
Pubchem ID :2455

Safety of YM-58483

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Calcium Channel

In Vitro:

Cell Line
Concentration Treated Time Description References
SU-DHL-4 cells 3 μM 30 minutes To investigate the effect of YM-58483 on BIRD-2-induced apoptosis, results showed that YM-58483 did not reduce BIRD-2-induced apoptosis PMC6214954
Human endometrial stromal cells (HESCs) 10 μM 6 days YM-58483 significantly decreased COX2, BMP2, and WNT4 transcript levels PMC5778154
Human B cells 50 nM 72 hours To investigate the effect of YM-58483 on B cell differentiation, results showed that YM-58483 suppressed B cell differentiation and reduced IgG production. PMC8569388
spinal astrocytes 3 μM YM-58483 significantly prevented the calcium influx induced by TG, indicating its inhibition of SOCE in spinal astrocytes. PMC4886427

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
DBA/1 mice Collagen-induced arthritis (CIA) model Oral 5 or 10 mg/kg Daily administration for 10 days YM-58483 significantly reduced the incidence of CIA, prevented the development of inflammation and pain hypersensitivity, and improved other symptoms of arthritis. PMC4459018
Mice Hindlimb ischaemia model Mini-osmotic pump 0.1 mg/kg/day Once daily for 3 or 7 days YM-58483 promoted post-ischaemic blood flow recovery by inhibiting TRPC6 channel activity, particularly in hypercholesterolemic models, where it significantly improved blood flow recovery and endothelial function. PMC10092707
Rats Aged rat coronary arteries In vitro administration 20 μM Single dose, 30 minutes exposure YM-58483 significantly inhibited 5-HT and ET-1-induced contractions in coronary arteries from aged rats and improved endothelium-dependent vasodilation in aged rat coronary arteries. PMC10487684
C57BL/6 mice CFA-induced inflammatory pain model, SNI-induced neuropathic pain model, formalin-induced spontaneous pain model Oral, intrathecal, intraplantar 10 mg/kg or 30 mg/kg Single administration, duration 1-3 hours To investigate the analgesic effects of YM-58483 in acute and chronic pain models. The results showed that YM-58483 significantly attenuated CFA- and SNI-induced pain hypersensitivity and reduced formalin-induced spontaneous nociceptive behavior. PMC3778044
Mice MRL/lpr lupus mice Intraperitoneal injection 1 mg/kg Once daily for 6 weeks To investigate the therapeutic effect of YM-58483 on lupus nephritis, results showed that YM-58483 ameliorated kidney damage, reduced the percentage of plasma cells in the spleen, and decreased the level of anti-double-stranded DNA antibodies in the serum. PMC8569388

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.87mL

2.37mL

1.19mL

23.73mL

4.75mL

2.37mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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