ABT-102 - CAS 808756-71-0
Catalog number:
808756-71-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C21H24N4O
Molecular Weight:
348.44
COA:
Inquire
Targets:
TRP Channel
Description:
ABT 102 is a selective transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with IC50 values to be 5-7 nM. No recent reports of development identified for phase-I development in Pain in USA.
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Purity:
98%
Appearance:
White solid
Synonyms:
1-[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-3-(1H-indazol-4-yl)urea
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
Pain
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Boiling Point:
No Data Available
Melting Point:
206 - 207℃
InChIKey:
TYOYXJNGINZFET-GOSISDBHSA-N
InChI:
InChI=1S/C21H24N4O/c1-21(2,3)14-8-9-15-13(11-14)7-10-18(15)24-20(26)23-17-5-4-6-19-16(17)12-22-25-19/h4-6,8-9,11-12,18H,7,10H2,1-3H3,(H,22,25)(H2,23,24,26)/t18-/m1/s1
Canonical SMILES:
CC(C)(C)C1=CC2=C(C=C1)C(CC2)NC(=O)NC3=CC=CC4=C3C=NN4
Current Developer:
Originator Abbott Laboratories
1.Effects of the TRPV1 antagonist ABT-102 on body temperature in healthy volunteers: pharmacokinetic/ pharmacodynamic analysis of three phase 1 trials.
Othman AA1, Nothaft W, Awni WM, Dutta S. Br J Clin Pharmacol. 2013 Apr;75(4):1029-40. doi: 10.1111/j.1365-2125.2012.04405.x.
AIM: To characterize quantitatively the relationship between ABT-102, a potent and selective TRPV1 antagonist, exposure and its effects on body temperature in humans using a population pharmacokinetic/pharmacodynamic modelling approach.
2.Formulation design and evaluation of amorphous ABT-102 nanoparticles.
Jog R1, Kumar S1, Shen J1, Jugade N2, Tan DC2, Gokhale R2, Burgess DJ3. Int J Pharm. 2016 Feb 10;498(1-2):153-69. doi: 10.1016/j.ijpharm.2015.12.033. Epub 2015 Dec 15.
Amorphous nanoparticles are able to enhance the kinetic solubility and concomitant dissolution rates of BCS class II and BCS class II/IV molecules due to their characteristic increased supersaturation levels, smaller particle size and greater surface area. A DoE approach was applied to investigate formulation and spray drying process parameters for the preparation of spray dried amorphous ABT-102 nanoparticles. Stability studies were performed on the optimized formulations to monitor physical and chemical changes under different temperature and humidity conditions. SLS/soluplus(®) and SLS/PVP K25 were the best stabilizer combinations. Trehalose was used to prevent nanoparticle aggregation during spray drying. Particle size distribution, moisture content, PXRD, PLM, FTIR and in vitro dissolution were utilized to characterize the spray dried nanoparticle formulations. The formulations prepared using soluplus(®) showed enhanced dissolution rate compared to those prepared using PVP K25.
3.The amorphous solid dispersion of the poorly soluble ABT-102 forms nano/microparticulate structures in aqueous medium: impact on solubility.
Frank KJ1, Westedt U, Rosenblatt KM, Hölig P, Rosenberg J, Mägerlein M, Fricker G, Brandl M. Int J Nanomedicine. 2012;7:5757-68. doi: 10.2147/IJN.S36571. Epub 2012 Nov 12.
Amorphous solid dispersions (ASDs) are a promising formulation approach for poorly soluble active pharmaceutical ingredients (APIs), because they ideally enhance both dissolution rate and solubility. However, the mechanism behind this is not understood in detail. In the present study, we investigated the supramolecular and the nano/microparticulate structures that emerge spontaneously upon dispersion of an ASD in aqueous medium and elucidated their influence on solubility. The ASD, prepared by hot melt extrusion, contained the poorly soluble ABT-102 (solubility in buffer, 0.05 μg/mL), a hydrophilic polymer, and three surfactants. The apparent solubility of ABT-102 from the ASD-formulation was enhanced up to 200 times in comparison to crystalline ABT-102. At the same time, the molecular solubility, as assessed by inverse equilibrium dialysis, was enhanced two times. Asymmetrical flow field-flow fractionation in combination with a multiangle light-scattering detector, an ultraviolet detector, and a refractometer enabled us to separate and identify the various supramolecular assemblies that were present in the aqueous dispersions of the API-free ASD (placebo) and of binary/ternary blends of the ingredients.
4.Pharmacokinetics of the TRPV1 antagonist ABT-102 in healthy human volunteers: population analysis of data from 3 phase 1 trials.
Othman AA1, Nothaft W, Awni WM, Dutta S. J Clin Pharmacol. 2012 Jul;52(7):1028-41. doi: 10.1177/0091270011407497. Epub 2011 May 12.
ABT-102 is a selective TRPV1 antagonist with robust efficacy in several preclinical models of pain. Three phase 1 studies evaluated ABT-102 pharmacokinetics upon oral administration to healthy human volunteers: a single-dose study (2, 6, 18, 30, and 40 mg) and a multiple-dose study (2, 4, and 8 mg twice daily for 7 days) using a solution formulation and a multiple-dose study (1, 2, and 4 mg twice daily for 7 days) using a solid-dispersion formulation. These studies followed double-blind, randomized, placebo-controlled designs. ABT-102 exhibited dose- and time-linear pharmacokinetics. ABT-102 half-life ranged from 7 to 11 hours, and steady state was achieved by day 5 of dosing. Population analysis of the pharmacokinetic data from the 3 studies was conducted. A 1-compartment model with a transit compartment for absorption and first-order elimination provided best fit to the data. The model included formulation-dependent lag times and a bioavailability factor (F(rel)) for solution relative to solid dispersion.
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CAS 808756-71-0 ABT-102

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