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A7361 2R, 4R-APDC monohydrate ≥98% (HPLC) 2R,4R-APDC is a Group II mGluR metabotropic glutamate receptor.
 
C9749   CBiPES hydrochloride ≥98% (HPLC) CBiPES is a positive allosteric modulator of the mGlu2 receptor. CBiPES attenuates stress-induced hyperthermia and blocks the hyperlocomotor effects of PCP in murine models. In rat brain, CBiPES attenuates ketamine-induced increase in extracellular histamine concentration. This compound is a sulfonamide, different chemical class from other mGlu2R agonists in the Sigma catalog.
 
C9847 Cyclothiazide Blocks the rapid desensitization of the AMPA glutamate receptors and markedly prolongs the decay time of the evoked excitatory post-synaptic current.
human ... CA1(759), CA4(762), GRIA1(2890), GRIA2(2891), GRIA3(2892), GRIA4(2893)
rat ... Gria1(50592)
D7071 Dapoxetine hydrochloride ≥98% (HPLC) Potent Selective serotonin reuptake inhibitor (SSRI); used in treatment of premature ejaculation
 
D5942 DAPT ≥98% (HPLC), solid DAPT is a γ-secretase inhibitor and indirectly an inhibitor of Notch, a γ-secretase substrate. Other γ-secretase substrates include LDL receptor-related protein, E-cadherin and ErbB-4. As an inhibitor of γ-secretase, DAPT may be useful in the study of β-amyloid (Aβ) formation. DAPT has been shown to inhibit Notch signaling in studies of autoimmune and lymphoproliferative diseases, such as ALPS and lupus erythematosus (SLE), as well as in cancer cell growth, angiogenesis, and differentiation of human induced pluripotent stem cells (hIPSC).
human ... APH1A(51107), APH1B(83464), NCSTN(23385), NOTCH1(4851), NOTCH2(4853), NOTCH3(4854), NOTCH4(4855), PSEN1(5663), PSEN2(5664), PSENEN(55851)
mouse ... Aph1a(226548), Aph1b(208117), Ncstn(59287), Notch1(18128), Notch2(18129), Notch3(18131), Notch4(18132), Psen1(19164), Psen2(19165), Psenen(66340)
rat ... Aph1a(365872), Aph1b(300802), Ncstn(289231), Notch1(25496), Notch2(29492), Notch3(56761), Notch4(406162), Psen1(29192), Psen2(81751), Psenen(292788)
D0676 Dobutamine hydrochloride ≥98% β1-Adrenoceptor receptor agonist.
human ... ADRB1(153)
F132 Fluoxetine hydrochloride solid Fluoxetine hydrochloride is a selective serotonin reuptake inhibitor and functions as an antidepressant. This drug works at presynaptic terminals where it prevents the reuptake of serotonin, resulting in the accumulation of serotonin in extracellular fluid at synapses.
Selective serotonin reuptake inhibitor; antidepressant.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
F1678 R-(−)-Fluoxetine hydrochloride >98% (HPLC), solid Selective serotonin reuptake inhibitor.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
F1553 S-(+)-Fluoxetine hydrochloride ≥98% (HPLC), solid Fluoxetine hcl (hydrochloride) is a selective serotonin reuptake inhibitor and functions as an antidepressant. This drug works at presynaptic terminals where it prevents the reuptake of serotonin, resulting in the accumulation of serotonin in extracellular fluid at synapses.
Selective serotonin reuptake inhibitor.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
G6423 Gemcitabine hydrochloride ≥98% (HPLC) Gemcitabine is a widely used antitumor agents in both clinics and research labs. It is an antineoplastic agent and antimetabolite.
 
L9919 LY2033298 ≥98% (HPLC) LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 potentiates ACh-M4 binding, with no effect at M1/3/5 receptors. LY2033298 can also bind to the M ACh receptor, and mediate either positive or negative allosteric effects depending on the ligand used to probe receptor activity.
 
L2545 LY225910 ≥98% (HPLC) Cholecystokinin is expressed in the gastrointestinal tract and the central nervous system. Cholecystokinin receptor type 2 (CCK2) is a GPCR that is highly expressed in brain and spinal cord. CCK2 is implicated in many brain processes, including mood, anxiety, and pain, through its modulation of GABA neurotransmission.

LY225910 is a potent, selective CCK2 antagonist. LY225910 blocks agonism of CCK2 by CCK-8S, the peptide agonist. LY225910 has been measured in multiple systems, including GABA efflux from cortical cultures, depolarization of spinal cord neurons (via potassium conductance), modulation of excitatory postsynaptic potentials (EPSPs) in nucleus accumbens slices, and enhancement of morphine analgesia.
 
L1920 LY255283 ≥98% (HPLC), powder LY255283 is a competitive leukotriene B4 receptor antagonist, with an IC50 of about 100 nM. It is somewhat selective for the BLT2 receptor, since IC50 values at the BLT1 receptor are >10 μM. LY255283 reduces airway obstruction in animal models of asthma.
 
SML0225 LY255582 ≥98% (HPLC) LY255582 inhibits the diet-associated increases in mesolimbic dopamine levels and reduces the consumption of highly-palatable food intake.
LY255582 is a centrally active opioid receptor antagonist (defined as an inverse agonist in 2011 JPET paper) that inhibited weight gain in obese Zucker rats over 30 days. It is more that 5-fold selective for mu opioid receptor compared to kappa opioid receptors and 13-fold selective over delta opioid receptors.
 
L6670 LY266097 ≥98% (HPLC), powder LY266097 is a selective 5HT-2B antagonist with a pKI of 9.7 for the human cloned 5-HT2B receptor and a 100-fold greater selectivity for 5-HT2B than the human 5-HT2C and 5-HT2A.
 
L6795 LY311727 ≥98% (HPLC), powder LY311727 is an orally active; potent secretory Phospholipase A2 (sPLA2; Group IIa) inhibitor.
 
L5295 LY 320135 ≥98% (HPLC) LY320135 is a potent CB1 receptor antagonist/inverse agonist (Ki = 141 nM) with greater than 70-fold selectivity over CB2 receptors (Ki > 10 μM). Structurally dissimilar from SR 141716A and AM 251. Shows weak binding to both 5-HT2 (Ki = 6.4 μM) and muscarinic receptors (Ki = 2.1 μM)
 
SML0010 LY-334370 hydrochloride hydrate ≥98% (HPLC), powder LY-334370 hydrochloride is a selective 5-HT1F receptor agonist.
LY-334370 modulates the transmission in the mouse trigeminal system and inhibits the neuronal responses within rat Sp5C by inhibiting c-Fos activation. It shows efficacy in aborting migraine attacks.
 
L1045   LY-354740 hydrate ≥98% (HPLC) LY-354740 is a highly selective and potent agonist of group II mGlu (metabotropic glutamate) receptors. It displays antianxiety and antiaddictive activity in vivo. It?s orally and systemically active. It is anxiolytic and inhibits symptoms of morphine withdrawal in morphine-dependent mice.
 
L2411 LY-367,265 Antidepressant, inhibits the serotonin transporter; 5-HT2A serotonin receptor antagonist.
human ... HTR2A(3356)
L4420 LY-367385 hydrochloride ≥98% (HPLC) LY-367385 is a selective metabotropic glutamate 1a receptor (mGlu1a) antagonist.
 
L1170 LY-487379 hydrochloride ≥98% (HPLC) LY-487379 is a positive allosteric modulator of the metabotropic glutamate receptor mGluR2. EC50 = 1.7 μM. LY-487379 shows no intrinsic agonist or antagonist activity at hmGluR2 and has no activity at human mGluR3. LY-487379 markedly potentiates glutamate-stimulated [35S]GTPγS binding in a concentration-dependent manner at hmGluR2, shifting the glutamate dose-response curve leftward by 3-fold and increasing the maximum levels of [35S]GTPγS stimulation. LY-487379 has anxiolytic effects in fear-potentiated startle. This activity profile is useful in all symptom domains of schizophrenia.
 
M5750 Menadione sodium bisulfite ≥95% (TLC) Menadione sodium bisulfite is a water-soluble form of menadione, which belongs to the Vitamin K class of compounds. These are necessary for the biosynthesis of prothrombin and other blood clotting factors. Menadione is a prothrombogenic compound and is used as a model quinone in cell culture and in vivo investigations.

Menadione has been shown to affect gap-junctional intercellular communication by mediation of tyrosine phosphorylation. Menadione has demonstrated cytotoxic activity against a variety of cell lines and can induce apoptosis in cultured cells, such as osteoclasts and osteoblasts, via elevation of peroxide and superoxide radical levels.

An HPLC method for detection of menadione sodium bisulfite in multivitamin formulations has been published. A chemiluminescence assay for menadione sodium bisulfite in pharmaceutical preparations and biological fluids has been reported.
 
N7261 Nortriptyline hydrochloride ≥98% (TLC), powder Tricyclic antidepressant that is a more potent inhibitor of the norepinephrine transporter (Ki = 3.4 nM) than the serotonin transporter (Ki = 161 nM). 5-HT2 serotonin receptor antagonist.
human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
O1141 Olanzapine ≥98% (HPLC) Olanzapine is a 5-HT2 serotonin and D1/D2 dopamine receptor antagonist.
 
R1402 Raloxifene hydrochloride solid Raloxifene is a selective estrogen receptor modulator (SERM); acts as an anti-estrogen in both breast and uterine tissue while being estrogenic in bone. May have efficacy against estrogen-sensitive cancers.
 
T7947 (R)-Tomoxetine hydrochloride solid Norepinephrine uptake blocker.
 
V1377 Vinblastine sulfate salt powder, ≥96% (HPLC) Plant alkaloid that inhibits microtubule assembly by binding tubulin and inducing self-association in spiral aggregates in a reaction that appears to be regulated by the C-terminus of β-tubulin and is enhanced by GDP and GTP. Depolymerizes microtubules. Arrests the cell cycle in G2/M-phase by blocking mitotic spindle formation. Triggers Raf-1 activation, phosphorylation of bcl-2-family proteins, induction of p53 expression, and apoptosis in several tumor cell lines. Substrate of Pgp and CYP3A4.
human ... TBCC(6903)
V4890 Vindesine sulfate salt hydrate ≥95% (HPLC) Microtubule inhibitor. Vindesine binds to and stabilizes tubulin, thereby preventing tubulin polymerization, preventing mitosis, and arresting cells in metaphase.