Featured New Products

Selective inhibitor of p38α and p38β₂
2908 l EO 1428
Displays no activity at p38γ, p38δ, ERK1/2 and JNK1. Inhibits production of inflammatory cytokines including IL-8, TNF-α, IL-6, IL-1β and IL-10.
Related Products: JX 401 SD 169 SB 203580

α7 and α9 selective nAChR antagonist
3119 l α-Conotoxin ImI
Displays no effect on α2β2, α3β2, α4β2, α2β4, α3β3 and α4β4 subunit combinations.
Related Products: α-Conotoxin MII PNU 282987 Methyllycaconitine citrate

Selective TRPA1 blocker
2896 l HC 030031
Antagonises AITC- and formalin-evoked calcium influx (IC₅₀ values are 6.2 and 5.3 μM respectively). Does not block currents mediated by TRPV1, TRPV3, TRPV4, hERG or Na_V1.2 channels.
Related Products: Icilin WS 3 WS 12

Selective non-transportable GlyT1 inhibitor
2789 l NFPS
Displays no activity on GlyT2 or the transport of proline, GABA or glutamate. Enhances the amplitude of the NMDA component of glutamatergic EPSCs.
Related Products: ALX 5407 hydrochloride Sarcosine

Hsp90 inhibitor
3061 l Macbecin I
Ansamycin antibiotic compound that exhibits antitumour and cytocidal activities. Displays higher affinity and potency than geldanamycin (Cat. No. 1368).
Related Products: 17-DMAG hydrochloride 17-AAG CCT 018159

Potent α3β2 and β3 subunit selective nAChR antagonist
1340 l α-Conotoxin MII
Displays > 200-fold selectivity for α3β2 over α2β2, α4β2 & α3β4.
Related Products: Dihydro-β-erythroidine hydrobromide (±)-Anatoxin A fumarate Methyllycaconitine citrate

Selective Ca_V2.3 blocker (R-type)
2945 l SNX 482
Antinociceptive; inhibits nociceptive C-fibre and Aδ-fibre-evoked neuronal responses.
Related Products: (±)-Bay K 8644 ω-Conotoxin GVIA ω-Conotoxin MVIIC

Selective inhibitor of ALK5, ALK4 and ALK7
2939 l A 83-01
IC₅₀ values are 12, 45 and 7.5 nM for ALK5, ALK4 and ALK7 respectively. Only weakly inhibits ALK-1,-2, -3, -6 and MAPK activity.
Related Products: D 4476 LY 364947 SB 431542

PI 3-kinase inhibitor
2814 l PI 828
IC₅₀ values are 0.098, 0.183, 0.227 and 1.967 for P110β, p110α, p110δ and p110γ μM respectively. Displays higher potency than LY 294002.
Related Products: LY 294002 hydrochloride PI 103 hydrochloride 740 Y-P

GABA_A receptor ligand
2733 l U 90042
Binds with comparable affinities to three receptor subtypes: α₁β₂γ₂, α₃β₂γ₂ and α₆β₂γ₂ (K_i values are 7.8, 9.5 and 11.0 nM respectively). Sedative/hypnotic compound.
Related Products: Muscimol (-)-Bicuculline methochloride U 93631

p90 ribosomal S6 kinase (RSK) inhibitor
2250 l SL 010-1
Does not inhibit upstream kinases such as MEK, Raf and PKC. Inhibits the growth of MCF-7 human breast cancer cells with no effect on the normal breast cell line.
Related Products: PD 98059 GW 5074 NSC 23766

Selective Na_V1.8 blocker
2976 l A 803467
Antinociceptive; potently attenuates mechanical allodynia in two models of neuropathic pain following i.p. administration.
Related Products: Tetrodotoxin citrate QX 314 Batrachotoxin

Selective CK1 inhibitor
2902 l D 4476
Displays > 20-fold selectivity over SAPK2/p38 and a much greater selectivity over all other protein kinases tested.
Related Products: Ellagic acid TBB

Potent and selective 5-HT_2C agonist
3041 l CP 809101
Displays antipsychotic activity; suppresses condition avoidance responding (CAR) and inhibits PCP and amphetamine-stimulated hyperactivity in rats following subcutaneous administration.
Related Products: SB 242084) WAY 161503 DOI hydrochloride

VGF-derived peptide
2341 l TLQP-21
Spans residues 556-576 of the precursor sequence. Protects cerebellar granule cells (CGCs) from serum and potassium deprivation-induced apoptosis.
Related Products: BDNF (human) GW 441756 NTR 368

Potent, allosteric mGlu₇-selective antagonist
2963 l MMPIP
Inhibits agonist-induced intracellular calcium mobilisation and cAMP accumulation (IC₅₀ values are 26 and 610 nM).
mGlu Related Products: AMN 082 L-AP4 LY 341495

Selective 5-HT_2C antagonist
2901 l SB 242084
Displays 158- and 100-fold selectivity over 5-HT_2A and 5-HT_2B receptors respectively. Brain penetrant; exerts anxiolytic-like activity.
5-HT₂ Related Products: RS 102221 SB 206553 WAY 161503

CRF₁ antagonist
2778 l Antalarmin
Suppresses CRF-induced ACTH secretion. Blocks CRF- and novelty-induced anxiety-like behaviour in animal models of anxiety.
CRF Related Products: CRF (human, rat) Astressin α-helical CRF 9-41

Endogenous ghrelin agonist
2951 l [Des-octanoyl]-Ghrelin, rat
Non-acylated, major circulating isoform of ghrelin that does not bind to the growth hormone secretagogue (GHS) receptor, nor induce growth hormone release.
Ghrelin Related Products: Ghrelin (rat) Ghrelin (human) [Des-octanoyl]-Ghrelin (human)

Highly selective, orally active ET_A antagonist
2942 l CI 1020
Antihypertensive; blocks ET-1-induced pressor responses following oral administration.
ET_A Related Products: BMS 182874 BQ-123 FR 139317

Selective P2X₇ antagonist
2972 l A 438079
Devoid of activity at other P2 receptors (IC₅₀ >> 10 μM). Possesses antinociceptive activity in models of neuropathic pain in vivo.
P2X Related Products: KN-62 NF 449 PPADs

Tubulin polymerisation inhibitor
1495 l Combretastatin A4
Antitumour, antiangiogenic and antimetastatic agent, in vitro and in vivo. Acts by inhibiting tubulin polymerisation (IC₅₀ = 2-3 μM).
Related Products: D-64131 Vincristine Taxol

Potent GPR55 receptor agonist
2797 l O-1602
Analogue of cannabidiol. EC₅₀ values are 13, > 30000 and > 30000 nM for GPR55, CB₁ and CB₂ receptors respectively). Induces activation of RhoA, cdc42 and rac1.
Cannabinoid Related Products: O-1918 Abn-CBD Palmitoylethanolamide

High affinity EAAT1 and EAAT2 blocker
2532 l TFB-TBOA
Displays no activity on a wide range of neurotransmitter receptors and transporters. Induces convulsions following i.c.v. administration in mice.
EAAT Related Products: DL-TBOA WAY 213613 Dihydrokainic acid

NPY Y₁ receptor antagonist
2707 l BIBP 3226
Produces an anxiogenic-like effect in rats following i.c.v. administration.
NPY Related Products: PD 160170 BIIE 0246 Neuropeptide Y (human, rat)

Selective, non-peptide CRF₁ antagonist
2779 l CP 154526
Blocks CRF-induced adenylate cyclase activation (K_i = 3.7 nM) and attenuates activation of the HPA axis by CRF. Displays anxiolytic-like activity in the rat elevated plus-maze test; brain penetrant.
CRF Related Products: NBI 27914 K 41498 Stressin 1

Selective 5-HT₇ antagonist
2726 l SB 258719
Displays > 100-fold selectivity over a range of other receptors. Reverses the hypothermic effect of 5-CT in mice following i.p. administration.
5-HT Related Products: LP 44 SB 269970 AS 19

TRPM8 agonist; cooling agent
2927 l WS 3
Cooling agent that is an agonist at TRPM8 receptors (EC₅₀ = 3.7 μM).
TRP Receptor Related Products: Icilin AMG 9810 SB 366791

5-HT₃ antagonist
2903 l Granisetron
Possesses potent antiemetic activity.
5-HT Related Products: Tropisetron SR 57227 Y-25130

Orally active, subtype-selective NR1A/NR2B antagonist
2782 l TCS 46b
IC₅₀ values are 5.3, 35000 and > 100000 nM for NR1A/2B, NR1A/2A and NR1A/2C receptor subtypes respectively.
NMDA Related Products: Ro 25-6981 Ro 04-5595 CCMQ

Potent and selective NOP antagonist
2598 l J 113397
Inhibits nociceptin/orphanin FQ-induced hyperalgesia in the mouse tail-flick test.
NOP Related Products: JTC 801 Trap 101 NNC 63-0532

Potent CXCR2 antagonist
2724 l SB 265610
Inhibits CINC-induced chemotaxis and attenuates neutrophil accumulation in inflammatory lung injury in vivo.
Chemokine Receptor Related Products: BX 513 SB 225002 RS 102895

GluR1/2 selective AMPA antagonist
2770 l Philanthotoxin 74
Subtype-selective AMPA receptor antagonist; inhibits GluR1/2 but not GluR2/3 receptors.
AMPA Related Products: YM 90K ZK 200775 (S)-AMPA

Dual 5-HT / noradrenalin reuptake inhibitor
2917 l Venlafaxine
Displays ~ 30-fold higher affinity for SERT than NET (K_i values are 82 and 2480 nM respectively). Antidepressant; increases swimming and climbing behaviour in the forced-swim test in rats.
Related Products: Lofepramine Sibutramine BTS 54-505

Dipeptidyl peptidase IV inhibitor
2783 l DPPI 1c
Increases plasma GLP-1 levels and improves glucose tolerance in diabetic mice following oral glucose challenge.
Other Protease Inhibitors: Cilastatin ZJ 43

Cytochrome P450 inhibitor
2705 l Liarozole
Inhibits several cytochrome P450 enzymes including aromatase (CYP19) and retinoic acid 4-hydroxylase (CYP26). Blocks retinoic acid metabolism (retinoic acid metabolism blocking agent, RAMBA).
Related Products: TMS Ketoconazole Retinoic Acid Related Products

Selective GnRH receptor antagonist
2730 l AG 045572
Suppresses testosterone and luteinising hormone (LH) levels in vivo.
GnRH Related Products: Nafarelin T 98475

Histone deacetylase inhibitor
2771 l M 344
Induces terminal cell differentiation and causes an increase in hyperacetylated histone H4.
HDAC Related Products: NSC 3852 Valproic acid 4-Phenylbutyrate

Mixed 5-HT_2A / D₂ antagonist
2865 l Risperidone
Atypical antipsychotic agent that displays mixed 5-HT_2A/D₂ receptor antagonism (K_i values are 0.4 and 3.13 nM respectively).
Related Products: Amperozide Melperone Clozapine

Selective Inhibitor of PTP1B
2754 l TCS 401
Displays > 200-fold selectivity over CD45 D1D2, PTPβ, PTPε D1, SHP-1, PTPα D1 and LAR D1D2.
Phosphatase Related Products: BVT 948 Sodium Orthovanadate Tautomycetin

Potent and selective sst₅ agonist
1980 l L-817,818
Displays > 8-fold selectivity over other sst receptors. Inhibits growth hormone release from rat pituitary cells (EC₅₀ = 3.1 nM).
sst Related Products: Seglitide Octreotide NNC 26-9100

Antagonist of neurosteroid potentiation of GABA_A
2681 l 17-PA
Selective antagonist of neurosteroid potentiation and direct gating of GABA_A receptors.
GABA Related Products: Ganaxolone (-)-Bicuculline methiodide Tracazolate

Selective A_2B antagonist
2752 l MRS 1754
K_i values are 1.97, 16.8, 403, 503, 570 and 612 nM for hA_2B, rA₁, hA₁, hA_2A, hA₃ and rA_2A receptors respectively.
A_2B Related Products: PSB 1115 MRS 1706 CV 1808

GABA uptake inhibitor
2747 l NNC 05-2090
Displays moderate selectivity for BGT-1. Anticonvulsive; inhibits sound-induced tonic and clonic convulsions in DBA/2 mice.

GABA Uptake Related Products: NNC 711 SKF 89976A CI 966

Toll-like receptor 7 (TLR7) agonist
2719 l RWJ 21757
Induces immune cell activation and increases cytokine production. Displays antitumour and antiviral activity in various animal models.
TLR7 Related Products: Caffeic acid phenethyl ester IMD 0354 IKK 16

Highly selective CB₂ agonist
2764 l Gp 1a
CB₂ receptor agonist that displays > 9800-fold selectivity over CB₁ receptors. Increases P-ERK1/2 expression in HL-60 cells in vitro.
CB₂ Related Products: L-759,633 L-759,656 CB 65

Potent and selective CXCR2 antagonist
2725 l SB 225002
CXCR2 chemokine receptor antagonist (IC₅₀ = 22 nM) that displays > 150-fold selectivity over CXCR1 receptors. Causes inhibition of IL-8 and GROα-mediated calcium mobilisation in HL60 cells (IC₅₀ values are 8 and 10 nM respectively). CXCR2 Related Products: ZK 756326 RS 504393 DAPTA

Potent and selective P2Y₆ agonist
2715 l 3-Phenacyl UDP disodium salt
Potent and selective P2Y₆ receptor agonist (EC₅₀ values are 7, > 1000 and > 10000 nM for P2Y₆, P2Y₂ and P2Y₄ receptors respectively).
P2Y₆ Related Products: MRS 2578

Selective AMPA antagonist
2701 l YM 90K hydrochloride
Displays 26-fold and > 440-fold selectivity over kainate and NMDA receptors respectively. Neuroprotective; delays neuronal death in a global ischaemia model and cerebral infarction in a focal ischaemia model.
AMPA Related Products: ZK 200775 GYKI 52466

Potent and selective VPAC₂ agonist
2711 l Bay 55-9837
Selective VPAC₂ receptor agonist (IC₅₀ values are 60, 8700 and > 10000 nM for VPAC₂, VPAC₁ and PAC₁ receptors respectively). Stimulates glucose-dependent insulin secretion in isolated human pancreatic islets.
VPAC₂ Related Products: [Ala^11,22,28]VIP