1. Others
    Neuronal Signaling
    GPCR/G Protein
  2. Estrogen Receptor/ERR
    Cannabinoid Receptor
  3. Ridaifen-B

Ridaifen-B (Synonyms: RID-B)

Cat. No.: HY-101995
Handling Instructions

Ridaifen-B (RID-B) is a potent antagonist of estrogen receptor α (ERα) with IC50 of 52.4 nM, a tamoxifen (HY-13757A) derivative. Ridaifen-B is a high affinity, selective, inverse agonist at CB2 receptor (Ki=43.7 nM) over 17 folds CB1 receptor (Ki=732 nM). Ridaifen-B modulates G-protein (IC50=300 nM) and adenylyl cyclase activity with potency values predicted by CB2 affinity (IC50=134 nM). Ridaifen-B has anti-inflammatory, anti-cancer, and anti-osteoclastogenic effects.

For research use only. We do not sell to patients.

Ridaifen-B Chemical Structure

Ridaifen-B Chemical Structure

CAS No. : 886465-70-9

Size Price Stock
5 mg USD 315 Ask For Quote & Lead Time
10 mg USD 510 Ask For Quote & Lead Time

* Please select Quantity before adding items.

Top Publications Citing Use of Products

View All Estrogen Receptor/ERR Isoform Specific Products:

View All Cannabinoid Receptor Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ridaifen-B (RID-B) is a potent antagonist of estrogen receptor α (ERα) with IC50 of 52.4 nM, a tamoxifen (HY-13757A) derivative[1]. Ridaifen-B is a high affinity, selective, inverse agonist at CB2 receptor (Ki=43.7 nM) over 17 folds CB1 receptor (Ki=732 nM). Ridaifen-B modulates G-protein (IC50=300 nM) and adenylyl cyclase activity with potency values predicted by CB2 affinity (IC50=134 nM). Ridaifen-B has anti-inflammatory, anti-cancer, and anti-osteoclastogenic effects[1][3].

IC50 & Target[1][2]

ERRα

52.4 nM (IC50)

CB2

43.7 nM (Ki)

CB1

732 nM (Ki)

In Vitro

Ridaifen-B (0-4 μM; 4-24 hours) damages the Jurkat cells in a dose-dependent manner within 4 hours, the IC50 rate is 4 μM. In a longer time, Ridaifen-B also injures Jurkat cells in a dose-dependent manner, similar to the previous results obtained with short-term (4-h), and the IC50 rate is about 0.4 μM[1].
Ridaifen-B (0-4 μM; 4-24 hours) induces cell apoptosis, it activates Caspase-3 in a time-dependent manner, as well as cleaved pro-Caspase-3 to active caspase-3 in ER-negative Jurkat cells[1].
Ridaifen-B (300 nM-1 μM) co-incubates with LPS significantly decreases the Emax of NO production to 19.4 μM, 22.0 μM, and 18.2 μM, respectively in RAW264.7 murine macrophages[1].
Ridaifen-B acts as an inverse agonist at CB2 receptors for modulation of G-protein activity. The potency of RID-B to modulate G-protein activation is examined by employing a non-hydrolyzable radioactive analogue of GTP, [35S]GTPγS, which hinds to G-proteins irreversibly when activated. The CB2 agonist CP-55,940 increases G-protein activation with an EC50 of 2.3 nM. However, RID-B decreases G-protein activation with an IC50 of 300 nM[2].
Consistent with modulation of G-protein activity, RID-B increases adenylyl cyclase activity in a concentration-dependent manner, elevating cAMP levels with an Imax of 398% and a potency (IC50) of 134 nM[2].

Cell Viability Assay[1]

Cell Line: Jurkat cells
Concentration: 0-4 μM
Incubation Time: 4 hours; 24 hours
Result: Damaged cell cell viability in both short- and long- term treatment.

Apoptosis Analysis[1]

Cell Line: Jurkat cells
Concentration: 4 μM
Incubation Time: 24 hours
Result: Induced jurkat cells apoptosis.
Molecular Weight

510.71

Formula

C₃₄H₄₂N₂O₂

CAS No.

886465-70-9

SMILES

CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN3CCCC3)C=C2)\C4=CC=C(OCCN5CCCC5)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Ridaifen-BRID-BEstrogen Receptor/ERRCannabinoid Receptoranti-inflammatoryanti-canceranti-osteoclastogenictamoxifenderivativeapoptosisInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Ridaifen-B
Cat. No.:
HY-101995
Quantity:
MCE Japan Authorized Agent: