Featured Products 2008

Highlighted products added to the Tocris Bioscience range during 2008

December 2008

mGlu2 positive allosteric modulator
3283 | LY 487379

Potentiates glutamate-stimulated [35S]GTPγS binding (EC50 values are 1.7 and > 10 μM for mGlu2 and mGlu3 receptors respectively). Devoid of any activity at mGlu5 and mGlu7 receptors.

Related Products: LY 379268 LY 354740 LY 341495
Potent and selective CRF1 antagonist
3212 | CP 376395

Ki values are 12 and >10000 nM for CRF1 and CRF2 receptors respectively. Attenuates CRF-induced activation of the HPA axis in vivo following i.v. administration. Orally active.

Related Products: NBI 27914 CP 154526 CRF (human, rat)
Potent and selective FAK inhibitor
3239 | PF 573228

IC50 = 4 nM. Displays 50-250-fold selectivity over other protein kinases. Blocks serum and fibronectin-directed migration and decreases focal adhesion turnover in vitro.

Related Products: LY 294002 Y-27632 Marimastat
Highly selective NPY Y1 receptor antagonist
2412 | BIBO 3304

IC50 values are 0.38 and 0.72 nM at human and rat receptors respectively. Displays > 2600-fold selectivity over Y2, Y4 and Y5 receptors. Inhibits NPY- and fasting-induced feeding in vivo following central administration.

Related Products: BIIE 0246 Neuropeptide Y (human, rat) [cPP1-7,NPY19-23,Ala31,Aib32,Gln34] -hPancreatic Polypeptide
Potent, positive allosteric mGlu4 agonist
3248 | VU 0155041

EC50 = 798 and 693 nM at human and rat mGlu4 receptors respectively. Active in in vivo models of Parkinson's disease following i.c.v. administration.

Related Products: (S)-3,4-DCPG AMN 082 MMPIP

November 2008

Highly selective group II mGlu agonist
3246 | LY 354740

EC50 values are 5.1 and 24.3 nM at mGlu2 and mGlu3 receptors respectively. Displays antianxiety and antiaddictive activity in vivo. Orally active.

Related Products: LY 379268 LY 341495 DCG IV
Selective 5-HT4 partial agonist
3089 | CJ 033466

Displays > 1000-fold selectivity for 5-HT4 over other 5-HT and D2 receptors. Exhibits gastroprokinetic effects in vivo following oral administration.

Related Products: RS 67333 Cisapride Mosapride
Selective, reversible FAAH inhibitor
3262 | JNJ 1661010

IC50 = 12nM. Brain penetrant and active in vivo.

Related Products: AACOCF3 LY 2183240 Palmitoylethanolamide
Potent TGF-βRI inhibitor
3269 | SD 208

Displays > 100 fold and > 17 fold selectivity over TGF-βRII and other common kinases respectively. Exhibits anti-inflammatory and antitumour activity.

Related Products: A 83-01 D 4476 LY 364947
Antiprion agent
3238 | TCS PrP Inhibitor 13

Potently inhibits protease-resistant prion protein (PrP-res) accumulation in two types of prion-infected mouse neuroblastoma (N2a) cell lines (IC50 = 3nM).

October 2008

Selective 5-ht5A antagonist
3188 | SB 699551

pKi values are 8.3 for 5-ht5A and < 6.0 for 5-HT1B/D, 5-HT2A, 5-HT2C, 5-HT1A and 5-HT7 receptors.

Related Products: 5-Carboxamidotryptamine maleate
Urotensin II (U-II) receptor antagonist
3162 | [Orn5]-URP

pEC50 = 7.24. Displays no agonist activity unlike other U-II/URP analogues. Inhibits the action of U-II in the rat aorta ring assay.

Related Products: (±)-AC 7954 hydrochloride Urotensin II (human)
Potent and selective 5-HT6 antagonist
3189 | SB 399885

Displays > 200-fold selectivity for 5-HT6 over other 5-HT receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human 5-HT6 receptors respectively).

Related Products: EMD 386088 hydrochloride SB 258585 hydrochloride
Potent and selective MC4R agonist
3032 | THIQ

IC50 values are 1.2, 761 and 2067 nM for human MC4R, MC3R and MC1R receptors respectively. Stimulates erectile activity in rats ex copula following systemic administration.

Related Products: HS 024 Melanotan II
Selective 5-HT1F agonist
3079 | LY 334370

Ki values are 1.87, 16.4, > 100 (IC50), 176, 189 and 281 (IC50) nM for 5-HT1F, 5-HT1A, 5-HT4, 5-HT1E, 5-HT1B and 5-HT1D receptors respectively. Displays antimigraine effects.

Related Products: LY 344864 hydrochloride BRL 54443

September 2008

Selective EGFR inhibitor
3000 | Iressa (Gefitinib)

Shows minimal activity against ErbB-2, KDR, c-flt, PKC, MEK and ERK-2. Blocks EGFR autophosphorylation and inhibits tumour growth in mice bearing a range of human xenografts.

Related Products: AG 1478 PD 158780 AG 490
High affinity 5-HT2B antagonist
3077 | LY 272015

Ki values are 0.75, 21.63 and 28.7 nM for 5-HT2B, 5-HT2C and 5-HT2A receptors respectively. Orally active.

Related Products: SB 204741 SB 206553 Altanserin
Positive allosteric modulator of α7 nAChR
2995 | NS 1738

Exhibits no substantial activity for α4β2, α3β3 and α1-containing receptors. Displays cognitive-enhancing properties in vivo.

Related Products: PNU 282987 Methyllycaconitine citrate PNU 120596
Selective V1b agonist
3127 | d[Leu4,Lys8]-VP

Ki values are 0.16, 64, 100 and 3800 nM for V1b, oxytocin, V2 and V1a receptors respectively. Displays weak antidiuretic, vasopressor and in vitro oxytocic activities.

Related Products: d[Cha4]-AVP SR 49059 [Arg8]-Vasopressin
Potent and selective inhibitor of iNOS
2866 | BYK 191023

IC50 values are 86, 17000, 162000 nM for iNOS, nNOS and eNOS respectively). Acts in an NADPH- and time-dependent manner. Active in vivo, reverses pathological hypotension in the rodent endotoxin model.

Related Products: AMT L-Canavanine 1400W

August 2008

Selective EGFR inhibitor
3000 | Iressa (Gefitinib)

Shows minimal activity against ErbB-2, KDR, c-flt, PKC, MEK and ERK-2. Blocks EGFR autophosphorylation and inhibits tumour growth in mice bearing a range of human xenografts.

Related Products: AG 1478 PD 158780 AG 490
High affinity 5-HT2B antagonist
3077 | LY 272015

Ki values are 0.75, 21.63 and 28.7 nM for 5-HT2B, 5-HT2C and 5-HT2A receptors respectively. Orally active.

Related Products: SB 204741 SB 206553 Altanserin
Positive allosteric modulator of α7 nAChR
2995 | NS 1738

Exhibits no substantial activity for α4β2, α3β3 and α1-containing receptors. Displays cognitive-enhancing properties in vivo.

Related Products: PNU 282987 Methyllycaconitine citrate PNU 120596
Selective V1b agonist
3127 | d[Leu4,Lys8]-VP

Ki values are 0.16, 64, 100 and 3800 nM for V1b, oxytocin, V2 and V1a receptors respectively. Displays weak antidiuretic, vasopressor and in vitro oxytocic activities. Related Products: d[Cha4]-AVP SR 49059 [Arg8]-Vasopressin

Potent and selective inhibitor of iNOS
2866 | BYK 191023

IC50 values are 86, 17000, 162000 nM for iNOS, nNOS and eNOS respectively. Acts in an NADPH- and time-dependent manner.

Related Products: AMT L-Canavanine 1400W

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