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Favipiravir

andreas — Tue, 14 Apr 2020 08:57:27 +0000

•Favipiravir is a novel antiviral drug now in clinical trials for the treatment of influenza.

•It acts as a pseudo purine nucleic acid in virus-infected cells.

•Favipiravir inhibits the RNA polymerase of many different RNA viruses.

•It blocks replication of many strains of influenza virus, including the H7N9 avian virus.

•Favipiravir is also active against many arena-, bunya-, flavi-, alpha-, picorna- and noroviruses.

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WAY 316606 HCl

andreas — Wed, 06 Jun 2018 09:16:01 +0000

Description	WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC₅₀ of 0.5 μM.
IC₅₀ & Target	IC50: 0.5 μM (sFRP-1)^[1]
In Vitro	The EC₅₀ of WAY-316606 for Wnt-Luciferase Activity from U2-OS Cells is 0.65 μM^[1]. WAY-316606 binds to secreted frizzled-related protein (sFRP)-1 inhibitor with a K_D of 0.08 μM and inhibits sFRP-1 with an EC₅₀ of 0.65 μM. WAY-316606 also binds to sFRP-2, albeit over 10 times weaker with a K_D of 1 μM. Using a fluorescence polarization binding assay that employs a fluorescent probe compound and purified human sFRP-1 protein in a competitive-binding format, the IC₅₀ for WAY-316606 is 0.5 μM^[2].
In Vivo	WAY-316606 increases bone formation when tested in a neonatal murine calvarial assay. WAY-316606 increases total bone area up to 60% in a dose-dependent manner with an EC50 of about 1 nM. WAY-316606 has good aqueous solubility, moderate to low inhibition of cytochrome p450 isozymes (3A4, 2D6, 2C9) and good stability in rat and human liver microsomes (t_1/2>60 min in each species). In female Sprague-Dawley rats, WAY-316606 exhibits high plasma clearance (77 mL/min/kg, greater than hepatic blood flow) following a single intravenous bolus dose (2 mg/kg), which results in a rapid decline of drug exposure in the plasma despite the route of administration^[2].

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RU58841-myristate

andreas — Wed, 06 Jun 2018 08:22:57 +0000

Acne and androgenetic alopecia are linked to androgen effects and therefore should improve following
topical application of antiandrogens. There`s a new antiandrogen prodrug, RU 58841–myristate
(RUM) for topical therapy. Almost devoid of affinity to the androgen receptor, as derived from investigations in the mouse fibroblast cell line 29t/GRt, RUM is rapidly metabolised to the potent antiandrogenRU 58841 by cultured human foreskin fibroblasts and keratinocytes, male occipital scalp skin Dermal papilla cells, and by cells of the sebaceous gland cell line SZ95. In order to improve a specific targeting of the hair follicle, RUM was loaded on solid lipid nanoparticles (SLN), which are already known to support dermal targeting effects. Physically stable RUM loaded SLN were produced by hot homogenization. Penetration/permeation studies carried out using the Franz diffusion cell proved only negligible permeation of reconstructed epidermis and excised porcine skin within 6 h, implying a more topical action of the drug. Targeting to the hair follicle using SLN was visualised by fluorescence microscopy, following the application of Nile Red labelled SLN to human scalp skin. Transmission electron microscopy (TEM) allowed to detect intact silver labelled SLN in porcine hair follicles of preparations applied to the skin for 24 h. RUM loaded SLN should be considered for topical antiandrogen therapy of acne and androgenetic alopecia.

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PGE2

kaneshopadmin — Fri, 19 May 2017 10:09:53 +0000

CAS 363-24-6

Purity >98%

Research use only

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OC000459 sodium

kaneshopadmin — Tue, 16 May 2017 19:19:34 +0000

Description

OC000459 is a potent and selective CRTH2/DP2 antagonist with IC50 of 13 nM. Phase 2.

Targets

DP2 ^[1]

13 nM

In vitro

OC000459 inhibits the binding of [³H]PGD2 to membranes from CHO cells transfected with human DP2 with K_i of 13 nM. OC000459 also displaces [³H]PGD2 from membranes from human Th2 lymphocytes with K_i of 4 nM. OC000459 antagonizes PGD2-mediated calcium mobilization in a concentration-dependent manner with IC50 of 28 nM in intact CHO cells expressing DP2. OC000459 inhibits chemotaxis of human Th2 cells in response to PGD2 (10 nM) with IC50 of 28 nM. OC000459 (< 3 μM) antagonizes the effect of PGD2 competitively in both the isolated leukocyte preparation and heparinized human whole blood. OC000459 inhibits eosinophil shape change responses to DK-PGD2 with IC50 of 11 nM. OC000459 (1 μM) inhibits the activation of Th2 cells and eosinophils in response to mast cell supernatants. ^[1]

In vivo

OC000459 administrated at doses of 2 mg/kg p.o. in the Sprague-Dawley rats shows plasma half-life of 2.9 hours, time that maximal plasma concentration is achieved of 1.3 hours, maximal plasma concentration achieved is 1.54 μg/mL. OC000459 orally administrated 0.5 hour before injection of DK-PGD2 leads to a dose-dependent reduction in blood eosinophilia with ED50 of 0.04 mg/kg in rats. OC000459 orally administrated 0.5 hour before injection of DK-PGD2 also leads to a dose-dependent inhibition eosinophil accumulation ED50 of 0.01 mg/kg in rats. ^[1] OC000459 (200 mg twice daily for 28 days) administrated in patients with moderate persistent asthma shows improvement in quality of life as analysed for both the Full Analysis (FA) population and the Per Protocol (PP) population. In those patients, OC000459 improves the night-time symptom scores, reduces the geometric mean sputum eosinophil count and respiratory infections. ^[2] OC000459 (200 mg twice daily) treatment inhibits the later asthmatic responses and the post allergen increase in sputum eosinophils in steroid naive asthmatic patients.^[3]

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