An Asc-1 inhibitor
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BMS 466442

Item No. 42075

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[5-methoxy-6-(phenylmethoxy)-1H-indol-2-yl]carbonyl]-1-(phenylmethyl)-L-histidine, methyl ester
CAS Number
1598424-76-0
Molecular Formula
C31H30N4O5
Formula Weight
538.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(C1=CC(C(N1)=C2)=CC(OC)=C2OCC3=CC=CC=C3)N[C@H](C(OC)=O)CC4=CN(CC5=CC=CC=C5)C=N4
InChi Code
InChI=1S/C31H30N4O5/c1-38-28-14-23-13-26(33-25(23)16-29(28)40-19-22-11-7-4-8-12-22)30(36)34-27(31(37)39-2)15-24-18-35(20-32-24)17-21-9-5-3-6-10-21/h3-14,16,18,20,27,33H,15,17,19H2,1-2H3,(H,34,36)/t27-/m0/s1
InChi Key
UUCAHZCMRZOTNF-MHZLTWQESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $32

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    5 mg

    $145

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    10 mg

    $176

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    25 mg

    $400

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    Product Description

    BMS 466442 is an inhibitor of Asc-type amino acid transporter 1 (Asc-1).1 It selectively inhibits Asc-1 in HEK293 cells expressing Asc-1 (IC50 = 36.8 nM) over 40 other transporters (IC50s = >10 µM). BMS 466442 (100 nM) inhibits serine, cysteine, glycine, and alanine import and cAMP-induced increases in the oxygen consumption rate (OCR) and decreases mitochondrial uncoupling protein 1 (UCP1) levels in primary human white and brown adipose cells.2 It decreases the number of malformed neurons and reduces contextual fear memory deficits in a mouse model of surgery-induced brain damage when intracerebroventricularly infused.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brown, J.M., Hunihan, L., Prack, M.M., et al. In vitro characterization of a small molecule inhibitor of the alanine serine cysteine transporter -1 (SLC7A10). J. Neurochem. 129(2), 275-283 (2014).

    2. Arianti, R., Vinnai, B.Á., Tóth, B.B., et al. ASC-1 transporter-dependent amino acid uptake is required for the efficient thermogenic response of human adipocytes to adrenergic stimulation. FEBS Lett. 595(16), 2085-2098 (2021).

    3. Tapanes, S.A., Arizanovska, D., Díaz, M.M., et al. Inhibition of glial D-serine release rescues synaptic damage after brain injury. Glia 70(6), 1133-1152 (2022).