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CAS RN: 1201643-08-4 | Product Number: D4898

BD140 [for Albumin binding assay]


Purity: >98.0%(GC)
Synonyms:
  • 4,4-Difluoro-1-methyl-3-(4-propoxystyryl)-4-bora-3a,4a-diaza-s-indacene
Documents:
25MG
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100MG
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Product Number D4898
Purity / Analysis Method >98.0%(GC)
Molecular Formula / Molecular Weight C__2__1H__2__1BF__2N__2O = 366.22  
Physical State (20 deg.C) Solid
Condition to Avoid Light Sensitive
CAS RN 1201643-08-4
Reaxys Registry Number 19925561
PubChem Substance ID 354333597
Specifications
Purity(GC) min. 98.0 %
Melting point 153.0 to 157.0 °C
Lambda max. 563.0 to 567.0 nm(CH2Cl2)
Molar extinction coefficient min. 10000(CH2Cl2, 563.0 to 567.0nm)
Human serum albmin (HSA) binding activity S/N ratio min. 10
Competitive avtivity in competitive drug Remaining fluorescein inensity max. 20 %
Non-competitive avtivity in non-competitive drug Remaining fluoresein intensity min. 80 %
Properties (reference)
Melting Point 155 °C
Maximum Absorption Wavelength 565(CH2Cl2) nm
GHS
Pictogram Pictogram
Signal Word Warning
Hazard Statements H315 : Causes skin irritation.
H319 : Causes serious eye irritation.
Precautionary Statements P264 : Wash skin thoroughly after handling.
P280 : Wear protective gloves/ eye protection/ face protection.
P302 + P352 : IF ON SKIN: Wash with plenty of water.
P337 + P313 : If eye irritation persists: Get medical advice/ attention.
P305 + P351 + P338 : IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing.
P362 + P364 : Take off contaminated clothing and wash it before reuse.
P332 + P313 : If skin irritation occurs: Get medical advice/ attention.
Related Laws:
Transport Information:
H.S.code* 2934.99-000
*This code is applied to the products when TCI exports from Japan and not for import in your country.
Application
Fluorescent Probes for the Characterization of Two Specific Drug Binding Sites on HSA

Human Serum Albumin (HSA) binds to a wide variety of drugs at two primary binding sites (I: blue and II: yellow), and can have a significant impact on their pharmacokinetics and pharmacological effects. The fluorescent probes, dansylamide (1) and dansylglycine (2) selectively interact with sites I and II, respectively.1,2) BD140 (3) also binds to drug binding site II specifically.3) Changes in probe fluorescence are analyzed by fluorescence titrations as a result of competitive displacement by drugs and pharmaceuticals. The pattern of fluorescent probe displacement by these reagents enabled the identification of two specific drug binding sites, which illustrates their usefulness for the characterization of the binding sites in HSA.

D4898,D5405,D5406

References


Application
Specific fluorescent probe binding to drug binding site 2 on human serum albumin (HSA)

Binding of BD140 to HSA is not inhibited completely or nearly by warfarin and phenylbutazone, which bind to HSA drug binding site 1. On the other hand, binding of BD140 to HSA is inhibited sufficiently by ibuprofen, flurbiprofen and triiodobenzoic acid, which bind to drug binding site 2. Thus, BD140 is available for checking whether drugs bind to HSA drug binding site 2.

[Assay Condition]
Buffer: 1% DMSO in phosphate buffer (pH7.2 - 7.5), HSA: 20 µM (50 µL/well), Drugs: each concentration (50 µL/well), BD140: 20 µM(50 µL/well), Incubation: 20-25°C for 30 min, Measurement: plate-reader; excitation=365 nm, emission=585 nm.

References


PubMed Literature


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