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New Products
January 2010
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 PAM of δ-containing GABAA receptors
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3679 | DS2
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EC50 = 142 nM for α4β3δ receptors. Displays no effects on GABA responses mediated by α4β3γ2 and α1β3γ2 receptors.
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Related Products: L-655,708 L-838,417 TB 21007
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Potent and selective P2X7 antagonist
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3701 | A 740003
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IC50 values are 18 and 40 nM for rat and human receptors respectively. Reduces nociception in animal models of persistent neuropathic and inflammatory pain.
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Related Products: AZ 10606120 GW 791343 Ro 0437626
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Potent and selective CCR3 antagonist
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3650 | SB 328437
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IC50 = 4 nM. Displays > 2500-fold selectivity over C5aR, LTD4, CCR7, CXCR1 and CXCR2 receptors. Inhibits eotaxin-, eotaxin-2- and MCP-4-induced Ca2+ mobilization.
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Related Products: BMS CCR2 22 RS 504393 UCB 35625
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Tankyrase inhibitor; inhibits wnt signaling
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3748 | XAV 939
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IC50 values are 0.011 and 0.004 μM for TNKS1 and TNKS2 respectively. Antagonizes wnt signaling via stimulation of β-catenin degradation and stabilization of axin.
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Related Products: PJ 34 DR 2313 NU 1025
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Selective TRPV4 ligands
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3745 | RN 1747 & 3746 | RN 1734
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RN 1747 is a selective TRPV4 agonist (EC50 values are 0.77, 4.0 and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively) and antagonizes TRPM8 at relevant concentrations (IC50 = 4 μM). RN 1734 is a selective TRPV4 antagonist (IC50 values are 2.3, 5.9 and 3.2 μM for hTRPV4, mTRPV4 and rTRPV4 receptors respectively).
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All new products this month
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A 740003,
Adaphostin,
Asenapine,
Bretazenil,
Cevimeline,
Corticosterone,
DS2,
Dimebon,
GSK 264220A,
Indibulin,
MDL 72527,
Reversan,
RF 9,
RN 1747,
RN 1734,
RU 58668,
Sarpogrelate,
SB 328437,
SKA 31,
UCPH 101,
XAV 939
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