Structure
(PDE2A-IN-1, CAS 2648290-28-0)
KRH-3955 hydrochloride Biochemical | KRH-3955 biochemical
KRH-3955 hydrochloride
Purity
98%
Synonyms
KRH-3955 hydrochloride; N/A; KRH-3955 biochemical
Purity/Purification
98%
CAS
2253744-59-9
Targets&IC50
SDF-1alpha-CXCR4:0.61 nM (IC50), X4 HIV-1 NL4-3:0.3-1.0 nM (EC50)
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
In vitro
KRH-3955 (10 mg/kg; a single p.o.) efficiently suppresses X4 HIV-1 infection in hu-PBL-SCID mice[1]. KRH-3955 (10 mg/kg; a single p.o.) exhibits moderate oral bioavailability (25.6%) and C max (86.3 ng/mL)[1]. KRH-3955 (10 mg/kg; a single i.v.) exhibits terminal elimination half-lives (99 h) due to high plasma clearance (3.9 liters/h/kg) combined with large volumes of distribution (374 liters/kg)[1]. Animal Model: C.B-17 SCID mice engrafted with human PBMCs and injected with infectious X4 HIV-1 (NL4-3)[1]. Dosage: 10 mg/kg. Administration: A single p.o. administration. Result: Four of five mock-treated mice were infected whereas only one of five mice treated with KRH-3955 was infected. Animal Model: Male Sprague-Dawley rats[1]. Dosage: 10 mg/kg (Pharmacokinetic Analysis). Administration: A single p.o. or i.v. administration. Result: Well absorbed and the absolute oral bioavailability in rats was calculated to be 25.6%. The half time (T 1/2) of 99.0+/-13.1 h. Stable in human hepatic microsomes, and no significant inhibition of CYP450 liver enzymes by this compound was observed.
Preparation and Storage
Powder: -20 degree C for 3 years
In solvent: -80 degree C for 2 years
In solvent: -80 degree C for 2 years
Structure
(PDE2A-IN-1, CAS 2648290-28-0)
Structure
(PDE2A-IN-1, CAS 2648290-28-0)
Structure
(PDE2A-IN-1, CAS 2648290-28-0)
Structure
(PDE2A-IN-1, CAS 2648290-28-0)
Related Product Information for KRH-3955 biochemical
KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1alpha binding to CXCR4 with an IC 50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC 50 of 0.3 to 1.0 nM.
References
1. Tresadern G, et al. [1,2,4]Triazolo[1,5-a]pyrimidine Phosphodiesterase 2A Inhibitors: Structure and Free-Energy Perturbation-Guided Exploration. J Med Chem. 2020 Nov 12;63(21):12887-12910.
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Product Notes
The KRH-3955 (Catalog #AAA228276) is a Biochemical and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "KRH-3955 hydrochloride, Biochemical" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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