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(R)-(-)-Gossypol acetic acid

Cat. No. M13527
(R)-(-)-Gossypol acetic acid Structure
Synonym:

AT-101 (acetic acid); (-)-Gossypol acetic acid; (R)-Gossypol acetic acid

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Biological Activity

(R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.

Chemical Information
Molecular Weight 578.61
CAS Number 866541-93-7
Solubility (25°C) DMSO 25 mg/mL
Storage -20°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jian-Hong Lin, et al. Biomolecules. Gossypol Acetic Acid Attenuates Cardiac Ischemia/Reperfusion Injury in Rats via an Antiferroptotic Mechanism

[2] Dorota K Flak, et al. Int J Nanomedicine. AT101-Loaded Cubosomes as an Alternative for Improved Glioblastoma Therapy

[3] Hongxia Lin, et al. J Pharm Biomed Anal. A validated HPLC assay for the determination of R-(-)-gossypol in human plasma and its application in clinical pharmacokinetic studies

[4] Natalie McGregor, et al. J Cell Biochem. AT-101 (R-(-)-gossypol acetic acid) enhances the effectiveness of androgen deprivation therapy in the VCaP prostate cancer model

[5] Robert D Loberg, et al. Neoplasia. In vivo evaluation of AT-101 (R-(-)-gossypol acetic acid) in androgen-independent growth of VCaP prostate cancer cells in combination with surgical castration

Related Bcl-2 Products
BAD (103-127) (human)

BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL.

Bim BH3, Peptide IV

Bim BH3, Peptide IV is a 26-residue peptide from BH3-only protein Bim, which belongs to the pro-apoptotic group of the Bcl-2 family of proteins.

Bax inhibitor peptide, negative control

Bax inhibitor peptide, negative control is a inhibitor of Bax.

Bad BH3 (mouse)

Bad BH3 (mouse) is a biological active peptide.

Bid BH3 (80-99)

Bid BH3 (80-99) is a biological active peptide.

  Catalog
Abmole Inhibitor Catalog




Keywords: (R)-(-)-Gossypol acetic acid, AT-101 (acetic acid); (-)-Gossypol acetic acid; (R)-Gossypol acetic acid supplier, Bcl-2, inhibitors, activators


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